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Abstract:
Cyclin-dependent kinases 4/6 play an important role in regulation of cell cycle, and overexpress in a variety of cancers. Up to now, new CDK inhibitors still need to be developed due to its poor selectivity. Herein we report a novel series of 4-(2,3-dihydro-1H-benzo[d] pyrrolo[1,2-a] imidazole-7-yl)-N-(5-(piperazin-1-ylmethyl) pyridine-2-yl) pyrimidin-2-amine anologues as potent CDK 4/6 inhibitors based on LY2835219 (Abemaciclib). Compound 10d, which exhibits approximate potency on CDK4/6 (IC50 = 7.4/0.9 nM), has both good pharmacokinetic characters and high selectivity on CDK1 compared with LY2835219. Overall, compound 10d could be a promising candidate and a good starting point as anticancer drugs. (C) 2018 Elsevier Ltd. All rights reserved.
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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN: 0960-894X
Year: 2018
Issue: 5
Volume: 28
Page: 974-978
2 . 7 0 0
JCR@2022
ESI Discipline: CHEMISTRY;
ESI HC Threshold:192
JCR Journal Grade:3
Cited Count:
WoS CC Cited Count: 24
SCOPUS Cited Count: 28
ESI Highly Cited Papers on the List: 0 Unfold All
WanFang Cited Count:
Chinese Cited Count:
30 Days PV: 4
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