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Parallel synthesis of acylsemicarbazide libraries: preparation of potent cyclin dependent kinase (cdk) inhibitors.

Abstract：

:Potent cyclin dependent kinase inhibitors were prepared using parallel synthesis methodology. Treating advanced intermediate 2 with a variety of hydrazides in DMSO at 80 degrees C for 30 min gave the desired acylsemicarbazides in good to excellent yield. Several compounds were active against cdk4/D1 and cdk2/E in the low nanomolar range. The SAR indicates a wide variety of substituents are tolerated at the acylsemicarbazide moiety.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Nugiel DA,Vidwans A,Dzierba CD

doi

10.1016/j.bmcl.2004.09.023

subject

Has Abstract

pub_date

2004-11-15 00:00:00

pages

5489-91

issue

22

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(04)01108-4

journal_volume

14

pub_type

杂志文章

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