RESEARCH

Protein Kinase Inhibitor Development

"Kinome" is a depository of promising drug targets - protein kinases, which control vast diversity of molecular interactions in cell life. Indeed, numerous reports describing the discovery of new pharmaceutical substances targeting protein kinases have been published during last few years. Some of these substances are being tested in clinical trials, some of them are already on the market.

Our Department has been involved in extensive research and development of inhibitors for various protein kinases:

Aurone derivatives

Novel CK2 inhibitors among benzylidenebenzofuran-3(2H)-one (aurone) derivatives have been identified. A series of aurones have been synthesized. These compounds are structurally related...

1,3-thiazole-5-carboxylic acid derivatives

Novel CK2 inhibitors among 1,3-thiazole-4-carboxylic acid derivatives have been identified using virtual screening. The most active compound 2-(3-Fluoro-phenyl)-4-methyl-1,3-thiazole...

4-aminothieno[2,3-d]pyrimidines

Novel CK2 inhibitors among 4-aminothieno[2,3-d]pyrimidines have been identified. The most active compounds obtained in the course of the research are...

2-aminopyrimidinones and their 6-aza-analogs

In order to find the new potent CK2 inhibitors 60 derivatives of 2-aminopyrimidinones and their 6-aza-substituted analogs were synthesized and tested in vitro. Among them, the most...

2-phenylisothiazolidin-3-one-1,1-dioxides

We have synthesized 40 new 2-phenylisothiazolidin-3-one-1,1-dioxide derivatives. The optimization based on biological screening data and molecular modeling resulted in a 10-fold increase...