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RESEARCH Protein Kinase Inhibitors

Protein Kinase Inhibitors

"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:

1,3-thiazole-5-carboxylic acid derivatives

protopopov sNovel 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...

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4-aminothieno[2,3-d]pyrimidines

CK2_nhtpNovel CK2 inhibitors among 4-aminothieno[2,3-d]pyrimidines have been identified. The most active compounds obtained in the course of the research are...

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2-aminopyrimidinones and their 6-aza-analogs

ck2_img_new2In 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...

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

ck2_im_new2We 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...

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N-phenylnaphthostyril-1-sulfonamides

fgfr1_im4_new1New class of FGFR1 kinase inhibitors with naphthostyril heterocycle has been identified. A series of N-phenylnaphthostyril-1-sulfonamides has been synthesized and tested in vitro. It was...

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Other kinase inhibitors research:

CK2 Inhibitors
2-phenylisothiazolidin-3-one-1,1-dioxides Image
We have synthesized 40 new 2-phenylisothiazolidin-3-one-1,1-dioxide...



 

FGFR1 Inhibitors
Oxindoles Image
Oxindoles are known class of inhibitors of RTK, including FGFR1. We perform...



 

ASK1 Inhibitors
Identification of 3H-naphtho[1,2,3-de]quinoline-2,7-diones as Inhibitors of ASK1 Image
Virtual screening and biochemical screening allowed us to identify...



 

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