International Symposium on Advances in Synthetic and Medicinal Chemistry
Kiev, Ukraine, August 23-27, 2009
ASMC09 Kiev was organized by European Federation for Medicinal Chemistry (EFMC) and ChemBridge Corporation as the 3rd in the series of events which started five years ago with ASCMC04 Moscow. The second symposium in the series was held in St. Petersburg in 2007. The idea of such a series of international scientific event in the field of organic and medicinal chemistry was created about five years ago aiming bringing together the leading scientists and expert practitioners from academic, government and industrial institutions of eastern and western countries to power up the scientific potential which stayed apart for a long time. For these reasons, the locations of the meetings were decided to be chosen from the eastern countries. Following the tradition, the third symposium was held in Kiev, the capital city of Ukraine, which also offered a pleasurable social and cultural experiences to the participants with its historical heritage and great museums.
The ASMC09 Kiev with its distinguished panel of 50 internationally renowned speakers from academia and the pharmaceutical industry as well as 130 peer reviewed poster presentations continued the tradition which resulted a great success in advancing science of medicinal and organic chemistry and also successfully created a network of international audience of about 300 delegates from all over the world hence promoting cooperation and exchange of ideas. This 3rd meeting of the symposium series was chaired by Prof. Eric Carreria (ETH, Zuirch, Switzerland) and Dr. Scott Biller (Novartis, Cambridge, USA) to create an environment for discussing emerging trends in synthetic organic and medicinal chemistry as well as novel approaches in drug design and recent advances in drug discovery and development.
The highlights of the symposium included:
- Case histories from chemistry to the recently developed clinical candidates
- Fragment inspired and structure guided medicinal chemistry
- Strategies for building focused small molecule screening libraries in drug discovery
- Novel synthetic and catalytic methodologies in natural products and heteroaromatic chemistry
The core structure of the symposium successfully brought together the synthetic organic and medicinal chemistry and carried a message that changing face of organic synthesis for making biologically important molecules has a pivotal role using medicinal chemistry approaches more efficiently in drug discovery process. Each session was organized in a heterogeneous way including talks for advanced methods in synthetic organic chemistry, use of structural biology, property- and structure-based approaches in drug discovery and real-life case studies for developing novel drug candidates. It was obvious that the symposium chairmen and the members of organizing committee have done a great job to invite speakers from both academia and pharmaceutical industry with particular care on didactic aspects of the symposium. Additionally, equal distribution of the speakers from both academia and industry ideally allowed audience to understand the current picture of drug discovery and development process with the newest technologies as well as the place of medicinal chemistry within the process.
The first day of the symposium emphasized the changing face of organic synthesis with presented novel methodologies in heterocyclic synthesis, C-C bond forming and C-H bond reactivity for streamlining the synthesis of more complex molecules with biological relevance. Harmonized with these talks also the structure-based approaches had its place with case histories of BACE inhibitors for Alzheimer’s disease, inhibitors of Gli1-mediated transcription as anticancer agents, bisubstrate COMT inhibitors for Parkinson disease, discovery of Ixabepilone, a natural product epothilone analogue, for metastatic breast cancer. The second day continued with more medicinal chemistry stories using fragment based approaches for turning fragments-to-leads. Especially, emphasize given to use the techniques associated with fragment- and structure-based drug discovery such as X-ray crystallography or NMR for structural understanding of the binding interactions between the fragments or structures and their target protein. Session topics included different protein families comprising kinases, ATPases, proteases, adenosine deaminase, Bcl-2, HIV-1 RT dimerization process inhibitors for treating various pathologies associated with these proteins. These talks followed by a Business Mini Symposium on how to create and use a medicinal chemistry screening libraries in drug discovery process. This mini symposium session covered the use of chemistry to constitute and maximize the potential of HTS small molecule libraries for providing a utility to determine novel drug-like molecules from vast chemical diversity for various range of target classes with the aim of a rational target-driven selection of compounds for further development. Third and fourth days of the meeting continued the same tradition with more case stories on different targets such as BCR-ABL kinase inhibitors, PPARα agonists, beta-2-adrenoreceptor agonists, PI3K inhibitors, BACE1 inhibitors, orexin receptor antagonists. These stories was very exciting in a way that although the use of modern approaches have widely been utilized to identify and understand the structural interactions of lead compounds for clinical development, the use of conventional and novel chemical strategies was the basic driven force for the success of each story.
By Erden Banoglu
Univ. Parma, IT
Gazi Univ., TR
Univ. of Geneve, CH
Univ. Halle-Wittenberg, DE
Univ. Copenhagen, DK
Gerhard Ecker President
Roberto Pellicciari Past-Pres.
Koen Augustyns Secretary
Rasmus P.Clausen Treasurer
Javier Fernandez Member
Mark Bunnage Member
Peter Matyus Member