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Identification and structure-activity relationship studies of 3-methylene-2-norbornanone as potent anti-proliferative agents presumably working through p53 mediated apoptosis.

Abstract：

:We have identified a novel series of alpha-methylene carbonyl compounds through structure-activity relationship (SAR) studies with high levels of anti-proliferative activities. The lead molecule, 3-methylene-2-norbornanone (3) showed potent activity (LC(50)=3-8 microM) against mutant p53 cell types and many fold selectivity (>13-29) over wild-type p53 cells. Further, compound 3 and its analogs showed refolding of mutant p53 protein comparable to their anti-proliferative activities suggesting possible interaction with mutant p53 protein.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Reddy NL,Hill J,Ye L,Fernandes PB,Stout DM

doi

10.1016/j.bmcl.2004.08.048

subject

Has Abstract

pub_date

2004-11-15 00:00:00

pages

5645-9

issue

22

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(04)01056-X

journal_volume

14

pub_type

杂志文章

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