Special Issue "Design and Study of Kinase Inhibitors"
Deadline for manuscript submissions: closed (31 July 2014)
Prof. Dr. Philippe Belmont
School of Pharmacy, University Paris Descartes, UMR CNRS 8638, case 24. 4, avenue de l’Observatoire, 75006 Paris, France
Interests: heterocyclic synthesis; nitrogen-containing heterocycles; methodologies using organic or organometallic reagents; organometallic catalysis; cyclo-isomerization reactions; cyclo-functionalization reactions; benzannulation; aminobenzannulation; pi-acid metal catalysis; silver chemistry; gold chemistry; cobalt chemistry; Pauson-Khand reaction; bioactive compounds; alkaloids; kinases inhibition
In recent years, the design and study of kinase inhibitors has become an important field of interest. The arrival of imatinib (Glivec®, Novartis) on the market in the early 2000s opened the way for targeted therapies with heterocyclic molecules. Meanwhile, heterocyclic chemistry has received increasing attention in organic and organometallic methodologies. The green chemistry development brought the community access to heterocycles through new, efficient, and eco-friendly methodologies, including novel chemical conditions (e.g., metal-catalyzed or metal-free) and the use of new reaction conditions (e.g., microwave, solvent-free). Thanks to co-crystallization data (when possible) and molecular modeling studies (including docking), the link between heterocycle synthesis and their kinases’ inhibitory properties (i.e., the structure-activity relationships) has been further elucidated and is nowadays increasingly predictable.Therefore, the Special Issue’s scope, which concerns the “design and study of kinase inhibitors”, is broad. Possible topics may concern original access to various heterocyclic cores (through creative methodological developments) and close collaborations with either biologists/crystallographers or molecular modeling partners that empower inhibitor development and the hit to lead maturation.
Prof. Dr. Philippe Belmont
Manuscript Submission Information
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- kinase inhibition
- signal transduction study
- organic synthesis
- organometallic catalysis
- molecular modeling