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Design, synthesis, and biological evaluation of novel 3-pyrrolo[b]cyclohexylene-2-dihydroindolinone derivatives as potent receptor tyrosine kinase inhibitors.

Abstract：

:A novel series of 3-pyrrolo[b]cyclohexylene-2-dihydroindolinone derivatives targeting VEGFR-2, PDGFR-β and c-Kit kinases were designed and synthesized. The molecular design was based on the SAR features of indolin-2-ones as kinase inhibitors. SAR study of the series allowed us to identify compounds possessing more potent inhibitory activities against the three kinases than sunitinb with IC50 values in the low nanomolar range in vitro. Additionally, some compounds also showed favorable antiproliferative activities against a panel of cancer cell lines (BXPC-3, T24, BGC, HEPG2 and HT29).

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Ding L,Tang F,Huang W,Jin Q,Shen H,Wei P

doi

10.1016/j.bmcl.2013.08.037

subject

Has Abstract

pub_date

2013-10-15 00:00:00

pages

5630-3

issue

20

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(13)00966-9

journal_volume

23

pub_type

杂志文章

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