Title: The 52<sup>nd</sup> International Conference on Medicinal Chemistry (RICT 2016) of the French Medicinal Chemistry Society (SCT) Held in Caen (Normandy)
Abstract: Outstanding Medchem in France: Guest editors Janos Sapi, Luc Van Hjfte, and Patrick Dallemagne look back at the 52nd International Conference on Medicinal Chemistry (RICT 2016) held in Caen, France. They discuss the history of the French Medicinal Chemistry Society (Société de Chimie Thérapeutique, SCT) and provide highlights of last year′s events, including some key presentations now collected in this Special Issue. The SCT is also involved in advancing medicinal chemistry by providing networking and training and by rewarding scientific excellence. The SCT develops scientific contacts with academic and industrial research teams, as well as chemistry and medicinal-chemistry-related federations and associations, on both the national and international level. The “Business Development” unit, created in 2015 under the guidance of Pascal George, with the mission to offer advice and assistance to small and medium-sized enterprises (SMEs) and biotech companies, has strengthened during the year with a number of additional experts. The activity has started and grown remarkably, with several contacts and contracts with SMEs. The International Conference on Medicinal Chemistry or “Rencontres Internationales de Chimie Thérapeutique” (RICT) is the flagship of our scientific activities. The first national congress of the SCT was held in Lille in 1965, a year before the foundation and official registration of the SCT. Organized annually, the RICT meetings bring together more than 25 internationally recognized speakers from Europe, America, and Asia, presenting cutting edge results and recent advances in modern drug discovery. Considered for many years a rather national meeting, the RICT opened progressively to a more international audience in the middle of the 1990s. In recent years, the SCT has gradually been transformed, becoming more dynamic, attractive, and visible. Since 2007, our RICT meetings have become truly international, and are now considered seminal events in medicinal chemistry. The conference language is exclusively English, and attendees from abroad have increased progressively from 25 % to more than 50 % (Nice in 2013 and Rouen in 2014, respectively). The significant number of French and foreign scientists, from academia and industry, illustrates that our annual congresses meet the expectations of the scientific community, and that the quality of our manifestations is recognized. Apart from this main scientific event, we hold One-Day Thematic Symposia and Workshops focused on special topics. For example, two symposia in 2013 and 2015 were devoted to the contribution of chemical biology to drug discovery, while a workshop in 2013 dealt with molecular diversity. For a couple of years now, the SCT has paid special attention to young researchers. Every year, a two-and-a-half-day meeting, called the Young Research Fellow Meeting is organized with the aim to offer an ideal incubator for new ideas, contacts, networks, and collaboration. The low registration fees and inexpensive accommodations make this high-level meeting perfectly accessible to young researchers. Moreover, a career session is included in the program which benefits students hoping to find employment in the medchem field. The SCT attributes awards and prizes to individuals and teams to encourage their research and their commitment to medicinal chemistry. The Paul Ehrlich Prize supported by Janssen R&D is given annually to researchers for their remarkable contribution to medicinal chemistry. The recently founded Pierre Fabre Award for Therapeutic Innovation recognizes scientific discoveries and innovative technologies resulting in substantial therapeutic breakthroughs in modern drug discovery. Our society also gives prizes to young researchers to encourage their activities in the field of therapeutic chemistry. Thus, special poster prizes with free registration to the American Chemical Society (ACS), European Federation for Medicinal Chemistry (EFMC), or RICT meetings are given to the best poster presentations. To promote excellence and to support young researchers at the beginning of their career, the SCT provides each year a prize entitled “Prix d'Encouragement à la Recherche en Chimie Thérapeutique”, sponsored by Institut de Recherches Servier. The transformations made recently in the SCT have solidified our activities, thus increasing our visibility and representation at the national and international level. The SCT is an active member of the EFMC, and Pascal George is a member of the Executive Committee, becoming its Treasurer since January 2015. The SCT is also present in the International Organizing Committee (IOC) of the next EFMC-International Symposium on Medicinal Chemistry (ISMC 2018) meeting to be held in Ljubljana (Slovenia). We have established collaborations with neighboring national societies as illustrated by a Joint Scientific Day organized with the Medicinal Chemistry and Chemical Biology Division of the Swiss Chemical Society (SCS) in 2015, at Dijon (Burgundy). Another congress, Frontiers in Medicinal Chemistry (FiMC 2016) was co-organized by the SCT, the Medicinal Chemistry Division of the German Chemical Society (GDCh), and the German Pharmaceutical Society (DPhG) in March 2016 in Bonn (Germany). The 52nd International Conference on Medicinal Chemistry (RICT 2016), entitled “Interfacing Chemical Biology and Drug Discovery“ was co-organized by the SCT and the University of Caen, on July 6–8, 2016, in Caen, Normandy (France). The symposium, held at Congress Center of Caen, gathered more than 370 attendees, coming from 38 countries, from across four continents, among which is an important number of Asian colleagues (25). Apart from France, the UK, Germany, and Spain were the three top represented nations. The Scientific Advisory Board, composed of internationally recognized colleagues, selected 23 plenary lectures, including two award lectures and eight oral communications of 30 min. The latter were presented by colleagues at the early stage of their independent research career. More than half of the speakers came from abroad (Europe 12, Asia 3, North America 2), equally from academia and industry. Nowadays academic and industrial research cannot be dissociated, and so we strived for a perfect mix of speakers from both worlds. The scientific program was completed with the presentation of more than 200 posters in two sessions. Local technical support and logistics were ensured by LD Organization and colleagues and students of CERMN (“Centre d′Etudes et de Recherche sur le Médicament de Normandie”), a research unit of the University of Caen, directed by Prof. Patrick Dallemagne. The main topics of this 52nd RICT meeting included the identification and validation of new targets, pathways, biomarkers, innovative diagnostic approaches, and tools to understand unravelling biological pathways for medicinal chemistry applications, as well as the presentation of new paths for exploring molecular space. Recent applications of chemoinformatics in drug discovery, new therapeutic approaches targeting the central nervous system (CNS), and case studies enhanced the program. After a short welcome ceremony, the scientific program was opened on Wednesday July 6, 2016 with the Paul Ehrlich Prize Lecture of Prof. Jean-Daniel Brion (University of Paris XI Châtenay-Malabry, France) who gave a stimulating talk on two research programs in oncology. The first part focused on the synthesis and biological evaluation of quinolinone-type novobiocin analogs targeting the heat-shock protein 90 (Hsp90), involved among others in folding and stabilization of tumor growth proteins. The second part was devoted to the design, synthesis, biological evaluation, and vectorization of new combretastatin A-4 analogs, acting as potent antimitotic and antivascular agents. In his lecture, Prof. Bernhard Küster (Technical University of Munich, Germany) gave a couple of examples of how human proteomes, the proteomics concept, and experiments may be useful in preclinical drug discovery. The second talk of the Target Identification session, delivered by Dr. Andrew Zhang (AstraZeneca R&D, Waltham, US), dealt with target deconvolution efforts to understand how previously identified thiadiazole analogs influence the Wnt signaling pathway. As part of the Chemical Biology session, the afternoon's program started with the talk of Prof. Edward Tate (Imperial College, London, UK), focusing on the new development of chemical biology tools, especially protein post-translational modifications, to validate potential drug targets in infectious diseases and in cancer. Additionally, he illustrated how new chemical tagging technologies may be useful as powerful analytical platforms for identification and quantification of protein lipidation in living cells and animals. These experiments provided a better insight into how lipidation changed in response to drug treatment and gave a new mechanism to quantify drug target engagement and selectivity in a complex living system. In the second talk of the session Dr. Minoru Yoshida (Riken Advanced Science Institute, Saitama, Japan) reported a novel role of SIRT2 in controlling the function of cortactin and eIF5a in response to growth signal and hypoxia, respectively. More precisely, SIRT2 deacetylates cortactin, an actin-binding protein, inducing cancer cell migration and metastasis. As illustrated by various examples, SIRT2 inhibition by chemical inhibitors almost completely blocked cortactin-mediated cell migration rendering this NAD+-dependent deacetylase as a promising target for anticancer therapy. The first talk of the Inflammation & Nociception session given by Dr. Alan Brown (Stratified Medical, London, UK) focused on the discovery of benzimidazole-type derivatives as potent and selective NAV1.8 (voltage-gated sodium channel) blockers for the treatment of pain. Subsequent optimization allowed the identification of a clinical candidate, PF-6305591, a potent and highly selective ion channel blocker, displaying excellent preclinical profile and ADMET properties. Dr. Sven Kühnert (Grünenthal GmbH, Aachen, Germany) presented identification and optimization experiments affording a set of selective, orally available and in vivo efficacious bradykinin 1 receptor (B1R) antagonists, as potential anti-inflammatory drugs. The first day of the congress ended with a welcome reception allowing attendees to discuss and network in a relaxed atmosphere. The second day's program, except for three talks in the morning, took place in parallel sessions offering attendees the possibility to choose from among various topics. With the first lecture Dr. Jan Hoflack (Oncodesign, Dijon, France) presented Nanocyclix®, an in-house medicinal chemistry technology allowing the generation of new probes and kinase inhibitors, based on small macrocycles including a hinge-binding motif and a macrocyclic linker. The CNS Targets session was made up of two plenary talks. In the first one, Dr. Santiago Rivera (CNRS/Aix-Marseille University, Marseille, France) reported that membrane-type 5-matrix metalloproteinase (MT5-MMP) deficiency provokes a significant and persistent amelioration of the pathological outcome of Alzheimer′s disease (AD), as illustrated by a drastic fall of beta amyloid (Aβ) level and neuroinflammation. The presented results evidenced MT5-MMP as a key enzyme in the control of amyloid precursor protein processing and cytokine signaling, and it may be a new potential target in AD treatment. Dr. Jean-Claude Ortuno (Institut de Recherches Servier, Croissy-sur-Seine, France) focused his talk on the design of selective dopaminergic D3 receptor antagonists with potent 5-HT6 affinity, opening up a promising path for improved treatment of schizophrenia. As part of the keynote lectures, organized in two parallel sessions, Dr. Nicolas Desroy (Galapagos, Romainville, France) reported on the discovery, ADMET, and pharmacokinetic optimization of autotoxin inhibitor GLPG1690, a clinical candidate for the treatment of idiopathic pulmonary fibrosis. Dr. Sylvie Claeysen (Institut Génomique Fonctionnelle/CNRS/INSERM/Université de Montpellier, Montpellier, France) gave a talk on the design of multitarget (AChE, 5-HT4, 5-HT6)-directed ligands to treat complex neurodegenerative diseases like AD. Continuing the case study session in the field of kinase inhibitors, Dr. Céline Cano (Newcastle Cancer Center, Newcastle-upon-Tyne, UK) presented the development of potent and highly selective dibenzothiophen-4-yl-cromenone-type DNA-dependent protein kinase inhibitors, displaying optimized physicochemical and pharmacokinetic properties. The newly founded Reaxys Award for Medicinal Chemistry, sponsored by Elsevier was awarded to Dr. Cano in recognition of the high quality of her results. The second talk of the Kinase session was given by Dr. Andras Kotschy (Servier Research Institute of Medicinal Chemistry, Budapest, Hungary) illustrating the merits and pitfalls of structure-guided drug discovery through two kinase projects. The afternoon's program in the Fragment-Based Drug Design session started with the keynote talk of Dr. Isabelle Krimm (CNRS/University of Lyon 1, Villeurbanne, France). She demonstrated how various NMR techniques may be considered as alternative tools in drug discovery to investigate weak protein–fragment interactions in case of failure of X-ray crystallography. Dr. Steve Durrant (Vertex Pharmaceuticals (Europe) Ltd, Abingdon, UK) reported on the fragment-based design of 3-aminopyrid-2-one-type potent and selective interleukin-2-inducible T-cell kinase (ITK) inhibitors with a potential application for the treatment of autoimmune and allergic diseases. In the Breakthrough in Therapeutics session, the keynote talk of Dr. Françoise Ochsenbein (CEA Saclay, Gif-sur-Yvette, France) focused on the design of midsize peptides (20–25 aminoacids) to inhibit protein–protein interactions between the histone chaperone Asf1 and histone H3-H4. In fact, a striking correlation was evidenced between high Asf1 (anti-silencing factor 1) expression level and the severity of breast cancers, making Asf1 a promising anticancer target. The second talk of the session was delivered by Dr. Sébastien Gouin (CNRS/University of Nantes, Nantes, France) on the design of mono and multivalent bacterial (E. coli) FimH antagonists and their in vitro/in vivo potential for the treatment of urinary tract infections and Crohn's disease. The plenary lecture of Prof. Young-Ger Suh (Seoul National University, Seoul, South Korea) presented in the Breakthrough in Therapeutics session, dealt with the development of novel antiangiogenic agents, applicable to treat retinal neovascularization. Dr. Oleg Melnyk (CNRS/University of Lille/Pasteur Institute of Lille, Lille, France) in his plenary lecture highlighted novel chemoselective ligation methods for protein total (or hemi) syntheses, aiming at the study of MET tyrosine kinase receptor activation mechanism and in fine the promotion of tissue regeneration or neoangiogenesis. Nowadays, new computational approaches have become indispensible to assist chemical biology and drug discovery projects. In this context, Dr. Bruno Villoutreix (INSERM/University Paris Diderot, Paris, France), in his plenary talk, illustrated how online computational tools may be used for the design of chemical probes, acting on emerging protein targets. Always in the Structure Based Drug Design session, the talk of Dr. Michael Hennig (LeadXPro AG, Villigen Switzerland) focused on recent advances in the application of biophysical methods for compound screening, hit identification–validation as part of structure-based drug discovery programs targeting membrane proteins. In the CNS Disorders session, the first lecture was delivered by Dr. Jean-Philippe Pin (CNRS/INSERM/University of Montpellier, Montpellier, France) dealing with the design of selective orthosteric and allosteric ligands, interacting with the mGlu receptor. It was also illustrated how mGlu receptor properties may be controlled by light-activated photoswitchable compounds. Dr. Michiel Van Gool (Janssen R&D, Toledo, Spain) was also interested in modulating metabotropic glutamate receptors (mGlu) by the design and optimization of allosteric site-binding derivatives. A gala dinner concluded the second day's program, welcoming the attendees in a beautiful medieval environment at the Domaine de la Baronnie. The third day of the symposium continued with two parallel plenary sessions. The Imaging session started with the lecture of Dr. Eva Jakab-Toth (CNRS, Orléans, France) on the design and physical properties of various lanthanide chelates as bimodal imaging agents for combined magnetic resonance imaging (MRI) and optical detection. The second talk of the session, made by Prof. Yasuteru Urano (The University of Tokyo, Tokyo, Japan), described the development of new hydroxymethyl rhodamine green (HMRG)-based fluorogenic probes for in vivo imaging of tiny tumors and time-lapse super-resolution imaging in living cells. In parallel, in the Molecular Diversity and Drug Efficiency session, Prof. Adam Nelson (University of Leeds, Leeds, UK) presented a talk on a novel discovery approach, called activitydirected synthesis (ADS), in which bioactive molecules emerge in parallel with associated syntheses to afford binding fragments, enabling a highly efficient exploration of chemical space. Dr. Mike Hann (GSK, Stevenage, UK) in his lecture pointed out how the control of “molecular obesity” (excessive lipophilic character) may influence cellular drug efficiency and in fine avoid premature demise of drug candidates. In the Case Study session, the lecture of Dr. Pascal Furet (Novartis Institute for Biomedical Research, Basel, Switzerland) provided an overview on the efforts at Novartis to identify and develop several small molecule drug candidates inhibiting p53–MDM2 protein–protein interaction. The second talk of the session, presented by Dr. James Henry (Eli Lilly & Co, Indianapolis, USA) focused on the discovery of LY3009120, a small-molecule-type pan-RAF inhibitor with minimal paradoxical pathway activation and resistance mechanisms, blocking proliferation in both BRAF and RAS mutant tumor cells. Dr. Alain Wagner (CNRS/University of Strasbourg, Illkirch, France), Laureate of the Pierre Fabre Award for Therapeutic Innovation 2016 in the closing lecture proposed a “scien-trepreneur journey from digital to in vivo organic chemistry”. He demonstrated how it is possible by bioorthogonal reactions to alter the molecular structure of drugs after its administration in living animals. By this methodology, it is possible to switch a substance from its bioactive to a bio-inert state, and concomitantly to switch from a long-life circulating compound to its fast excretion state. At the end of the meeting, a total of seven poster prizes were awarded. The two “Vocation for Medicinal Chemistry” prizes, supported by the “Institut de Recherches Servier” went to Sae Rin Jean (University of Toronto) and Honorine Lebraud (Astex Pharmaceuticals, UK) with an invitation to deliver a lecture at the SCT Young Research Fellow Meeting (JJC 2017), held in February 2017 in Châtenay-Malabry. Five poster prizes sponsored by ChemMedChem, went to Matthias Urfer (University of Zürich), Mélanie Roche (University of Paris XI), Maud Bollenbach (University of Strasbourg), Thibault Tintillier (University of Montpellier), and Jean-Pierre Jourdan (University of Caen). All five poster prize winners received free registration to the RICT 2017 meeting, a Wiley-VCH book of their choice, and a year-long subscription to ChemMedChem. The RICT 2016 meeting offered a dense scientific program with high-level talks covering the main fields of modern medicinal chemistry. The symposium provided an excellent opportunity for discussions, networking, academic and industrial exchanges, and a platform for sponsors and exhibitors to present their services and activities. Highlights of the successful conference can be seen in Figures 1 and 2. Highlights from RICT 2016. a) Caen Convention Center lobby during registration. b) Exhibition hall where meals and poster sessions were held. c) Plenary lecture hall with more than 300 attendees. (Photos courtesy of the official LDO photographer Fabien Venturi/RICT 2016 website.) Highlights from RICT 2016. a) Paul Ehrlich Prize recipient Jean-Daniel Brion with Luc van Hijfte (L) and Magali Motte (R). b) Pierre Fabre Award for Therapeutic Innovation recipient Alain Wagner with Janos Sapi (L) and Frédéric Marion (R). c) Reaxys Award for Medicinal Chemistry recipient Céline Cano with Janos Sapi (L) and Olivier Barberan (R). d) ChemMedChem poster prize winners Matthias Urfer, Mélanie Roche, Maud Bollenbach and, Thibault Tintillier. Not in picture are poster prize winner Jean-Pierre Jourdan and Vocation for Medicinal Chemistry awardees Sae Rin Jean and Honorine Lebraud. e) Gala dinner at the Domaine de la Baronnie. (Photos courtesy of the official LDO photographer Fabien Venturi /RICT 2016 website.) This Special Issue of ChemMedChem aims to offer a representative overview of the most recent scientific advances presented in different forms during the RICT 2016 meeting. We were pleased to find that a good number of speakers and poster presenters accepted our invitation to prepare an article covering the six main topics of the symposium and now present 15 outstanding papers here. This Special Issue includes a Review article, two Minireviews, three Communications and nine Full Papers. In their Review article, Dr. Margherita Di Pisa and Prof. Oliver Seitz (DOI: 10.1002/cmdc.201700266) give a general overview of nucleic-acid-templated reactions for the in situ synthesis and uncaging of bioactive molecules and nucleic acid imaging. Due to the recent progress in this field, this kind of templated reactions proceed with high chemoselectivity and turnover to trigger a sufficient quantity of product for selective protein interaction in complex biological media such as cells, lysates, or serum. As the authors emphasized, RNA-directed synthesis paved the way to cellular delivery of bioactive compounds, enabling in the near future a controlled targeting and drug distribution with reduced side effects in cancer therapy. In the first Minireview, Dr. Eva Jakab-Toth and Dr. Sara Lacerda (DOI: 10.1002/cmdc.201700210) present the state-of-the-art on the design and application of lanthanide complexes in MRI and theranostics. They provided an in-depth analysis on mechanistic aspects that enable the modulation of MRI and the design of responsive agents. Different theranostic strategies to monitor drug release from liponanoparticles or to deliver photosensitizers were also described. The selected examples illustrate the utility of innovative imaging and theranostic agents to give a better insight into physiological mechanisms, to contribute to target identification/validation, or to offer individualized medicine. In the second Minireview, Dr. Céline Cano and colleagues (DOI: 10.1002/cmdc.201700143) report the progress achieved in the field of the design and development of reversible and irreversible small molecule inhibitors of DNA-dependent protein kinase (DNA-PK), a key protein involved in the reparation of DNA double-strand breaks, representing a promising target in anticancer therapy. The first Communication deals with the highly challenging allosteric drug discovery. High selectivity, limited interaction with basic cellular physiological processes, and modulating (rather than inhibiting) protein activity are the main arguments for the recent development of allosteric ligands. Dr. Isabelle Krimm (DOI: 10.1002/cmdc.201700064) reports a new NMR method called 1D saturation transfer difference (STD) to identify allosterically bound pockets and the impact of ligands on allosteric transitions (protein dynamics/conformation changes). The method is particularly versatile for the detection of weak protein–ligand interactions especially in lack of X-ray crystallography. The second Communication is contributed by a research team from Janssen at Toledo, led by Dr. Michiel Van Gool (DOI: 10.1002/cmdc.201700101), on metabotropic glutamate receptors (mGlu2) modulators. Indeed, inhibition of mGlu2 with negative allosteric modulators is proven to be beneficial to the treatment of neurological disorders. They published a structure–activity relationship (SAR) study starting from a submicromolar 1,3,5-trisubstituted pyrazole-type lead compound to arrive to one-digit nanomolecular analogs in in vitro tests. From complementary pharmacological experiments they evidenced a correlation between in vitro potency, free brain concentration, and ex vivo receptor occupancy, to open up the path for further optimization studies. In the third Communication the research group of Caen, led by Prof. Christophe Rochais and Prof. Patrick Dallemagne (DOI: 10.1002/cmdc.201700102), describes the synthesis and biological evaluation of a series of new benzylphenylpyrrolizinones, showing enhanced radical scavenging and β-amyloid aggregation inhibition properties. Among the Full Papers, two focus on target identification/validation topics: Dr Andrew Zhang and co-workers (DOI: 10.1002/cmdc.201700028, featured on the front cover), report an integrated target deconvolution approach combining chemoproteomics and biochemical and cell biology techniques to indentify the intracellular target and the mechanism of action of a series of 1,2,3-thiadiazole-5-carboxamide analogs, as putative Wnt signaling pathway inhibitors. Dr. Dominique Bonnet and colleagues (DOI: 10.1002/cmdc.201700106), describe the design, preparation, and characterization of potent, sensitive, and high-quality (excellent signal-to-noise ratio) probes for a time-resolved FRET cell-based binding assay to investigate ligand–apelin receptor interaction at the cell surface. A few articles deal with cancer-related topics: Dr. Andras Kotschy and co-workers (DOI: 10.1002/cmdc.201600539) propose a structure-based drug discovery program for the development of new β-carboline-type DYRK1A kinase-selective derivatives. Harmine, a natural product with dual activity was submitted to X-ray crystallography-mediated pharmacomodulations in C-7, indole NH, and C-1 positions to afford DYRK1A-selective (vs. MAO-A) inhibitors. In the second article, Prof. Jean Guillon and colleagues (DOI: 10.1002/cmdc.201700049), in continuation of their previous work on the pyrrolo[1,2-a]quinoxaline pharmacophore, report the synthesis and antiproliferative activity of fifteen analogs. These analogs bear various imidazole or triazole-substituted 4-(piperidin-1-yl)benzyl side chains on the pyrrolo[1,2-a]quinoxaline ring system. Selecting appropriate starting materials, the proposed linear path enabled a high molecular diversity required for SAR studies. Biological evaluations against five leukemia cell lines (Jurkat, U266, K562, U937, and HL60) displayed interesting cytotoxic potential in general, with low micromolar inhibition (IC50=1-3 μm) for three derivatives, with low toxicity toward normal hematopoietic cells. The remaining five papers may be commonly identified as structure-based approaches, taking examples from cancer, cardiovascular, and infection diseases as main therapeutic areas. Prof. Philippe Cotelle and his team (DOI: 10.1002/cmdc.201700063) publish the synthesis and pharmacological evaluation of several hexasubstituted dipyrrins, involved as potential inhibitors of transcriptional co-activators YAP and TAZ. Oncogenic YAP and TAZ are the downstream effectors of the Hippo pathway interacting with TEAD, to regulate cell proliferation and tissue and organ size growth. Disrupting the YAP/TEAD association is considered as a valuable strategy in cancer therapy. Prof. Farzad Kobarfard and co-workers (DOI: 10.1002/cmdc.201700123) share their results on the design, synthesis, and biological evaluation of various 1-(arylideneamino)-4-aryl-1H-imidazole-2-amine derivatives displaying antiplatelet activity. Metallo β-lactamases (MBL), produced by important Gram-negative pathogens, are mono- or di-zinc metalloenzymes, responsible for hydrolyzing all classes (except monbactams) of β-lactams. Dr. Jean-François Hernandez and colleagues (DOI: 10.1002/cmdc.201700186) report the synthesis and biological evaluation of a large collection of 1,2,4-triazol-3-thione-type derivatives, from which several displayed micromolar inhibitory potency. Dr. Sébastien G. Gouin et al. (DOI: 10.1002/cmdc.201700061) present the physicochemical tuning of antiadhesives against E. coli by microencapsulation and methylene homologation. By preparing novel and more stable thiazolylaminomannosides (NeoTazMan) and their consequent microencapsulation in γ-cyclodextrin, water solubility is improved without compromising the antiadhesive effect against adherent-invasive E. coli (which promotes inflammation in patients with Crohn′s disease). Profs. Bernhard Kuster, Harald Schwalbe, Guillaume Médard, and colleagues (DOI: 10.1002/cmdc.201700217) highlight how a chemoproteomics-aided approach may be useful for the discovery of receptor tyrosine kinase EPHA2 inhibitors. Dasatinib, a clinical dual BCR-ABL/SRC inhibitor, was selected as starting point. Co-crystallization of Dasatinib with EPHA2, combined with docking experiments, revealed ATP pocket entrance and a ribose pocket, both amenable for chemical modifications. A SAR study supported by X-ray crystallography delivered detailed protein–inhibitor interactions allowing in fine the identification of a candidate, bearing a 3,5-bis(morpholino)aniline group instead of the substituted aminopyrimidine ring of Dasatinib. The year 2017 is already shaping up well with the society′s forthcoming events: The 24th edition of the Young Research Fellow Meeting (JJC 2017) took place from February 8th to 10th in Châtenay Malabry (University of Paris XI). This was a great success, giving the opportunity to more than 230 PhD students and postdocs registered from 23 countries to present their results in 25 oral communication and poster sessions. This meeting provides a unique occasion for attendees to present their work, exchange ideas with peers, and meet human resources representatives of pharmaceutical companies, small biotechs, and start-ups. At the meeting, special working groups were organized to help participants improve their CVs, with simulated job interviews and round-table discussions on career orientation. The 53rd International Conference on Medicinal Chemistry (RICT 2017) will be held from July 5th to 7th in Toulouse (Occitanie) with the theme “Drug Discovery and Selection” (Figure 3). The scientific program is organized around six main topics, as follows: The 53rd International Conference on Medicinal Chemistry (RICT 2017) will be held in Toulouse (Occitanie) from July 5th to 7th, 2017. Immunotherapy–Oncology Emerging & Neglected Diseases Breakthrough in Technologies for Drug Discovery Tackling the Delivery of Biologics Access to Novel Molecular Entities Case Studies To date, 29 internationally renowned speakers have confirmed their participation. As with the previous editions of RICT, the 21 plenary talks, including the Paul Ehrlich Prize and the Pierre Fabre Award Lectures will be completed by 8 keynote lectures. More than half of the speakers come from abroad (Germany 5; UK 4; Belgium 3; USA 2; Switzerland 2; and The Netherlands, China, Singapore, and Sweden with 1 speaker) with slightly more than half from academia (17 vs. 12 from industry). The Paul Ehrlich Prize 2017 has recently been conferred on Prof. Benjamin Davis (University of Oxford, UK) for his outstanding results on the chemical understanding and exploitation of biomolecular function with an emphasis on carbohydrates and proteins. The Scientific Committee of the RICT 2017 ensures the high quality and diversity of the scientific program together with the accessibility of the meeting to PhDs, postdocs, and local master students. For the latter, an advantageous registration fee is offered. Looking further ahead, a Fall One-Day Symposium entitled “Chemical Biology: Contribution to Molecular Therapeutic Innovation. Conjugates and Drug Discovery Chemistry: New Challenges for Targeted Therapies” will take place in Paris on December 7th with the participation of seven outstanding speakers. The aim of the symposium is to illustrate the great potential and the applications of conjugates in contributing to therapeutic innovation. In 2018, the 25th edition of Young Research Fellow Meeting (JJC 2018) will be held from March 5th to 7th in Orléans. The 54th International Conference on Medicinal Chemistry (RICT 2018) will then move to the beautiful city of Strasbourg, in Alsace from July 4th to 6th, 2018 (Figure 4). The 54th International Conference on Medicinal Chemistry (RICT 2018) will be held in Strasbourg (Alsace) from July 4th to 6th, 2018 Finally, we would like to thank ChemMedChem for the opportunity to present the French Medicinal Chemistry Society (SCT), one of most active among the national adhering organizations (NAOs) of the EFMC, and we hope to welcome you to our forthcoming scientific events. Prof. Janos Sapi Dr Luc Van Hijfte Prof. Patrick Dallemagne Janos Sapi is a Professor of Medicinal Chemistry and Vice Director of the “Institut de Chimie Moléculaire de Reims”, a CNRS research unit at the University of Reims Champagne-Ardenne. His research interest focuses on the synthesis of natural products and their analogs of biological interest, the design of enzyme inhibitors for kinases, metalloproteinases, and telomerase, and the development of new synthetic methods (tandem reactions, multicomponent approaches, radical reactions) towards molecular diversity. He obtained his PhD in organic chemistry from the Technical University of Budapest, Hungary in 1982. Prof. Sapi is author of more than 80 publications, co-inventor of 12 patents, and has given numerous invited lectures and seminars. He was the president of the French Medicinal Chemistry Society (SCT) between January 2015 and December 2016. Luc Van Hijfte has over 25 years of industrial experience in the area of drug discovery in the pharmaceutical industry. Since October 2016, he has been president of Novithera, a start-up active in the application of kinase inhibitors for cancer immunotherapy. Before taking up his new role at Novithera, he was the Chief Scientific Officer of NovAliX since 2012, where he was instrumental in the development of the internal programs that are licensed by Novithera. Prior to joining NovAliX, he was Head of Medicinal Chemistry Europe for Janssen R&D (J&J) and Research Director at Janssen Cilag France. Before that, he held different positions at Merrell Dow, HMR, and Sanofi. Dr. Van Hijfte obtained a PhD in organic chemistry from Gent University, Belgium. He is the author of over 100 publications, communications, and patents. He has been involved in numerous compounds reaching clinical development, of which one compound, Bedaquiline (Sirturo), for tuberculosis treatment, has reached the market. He is the president of the French Medicinal Chemistry Society (SCT) for the period 2017–2018. Patrick Dallemagne, PharmD, PhD, is a Professor of medicinal chemistry and currently the Dean of the Centre d′Etudes et de Recherche sur le Médicament de Normandie at the University of Caen, Normandy, France. His research interests lie in the field of drug design in oncology and neurosciences and are especially, currently dedicated to the discovery of multitargeted directed ligands with pleiotropic therapeutic interest against Alzheimer′s disease (AD). Within this frame, he recently, noticeably succeeded in the design of Donecopride, the first dual 5-HT4R agonist/AChE inhibitor, currently under preclinical investigation as a potential novel treatment for AD. Patrick is the co-author of more than 120 publications, has applied for eight patents, and has delivered more than 50 invited lectures and seminars.