期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 18, 期 5, 页码 1844-1853出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.01.042
关键词
Kinase; Cyclin dependent kinases; CDK; Kinase inhibitor; Tumor cell proliferation inhibition; Cell cycle; Anti-cancer
We have recently reported CDK inhibitors based on the 6-substituted pyrrolo[3,4-c]pyrazole core structure. Improvement of inhibitory potency against multiple CDKs, antiproliferative activity against cancer cell lines and optimization of the physico-chemical properties led to the identification of highly potent compounds. Compound 31 (PHA-793887) showed good efficacy in the human ovarian A2780, colon HCT-116 and pancreatic BX-PC3 carcinoma xenograft models and was well tolerated upon daily treatments by iv administration. It was identified as a drug candidate for clinical evaluation in patients with solid tumors. (C) 2010 Elsevier Ltd. All rights reserved.
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