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Updated: Aug 21, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Identification and structure-activity relationship studies of 3-methylene-2-norbornanone as potent anti-proliferative
N Laxma Reddy1, Jeanette Hill, Long Ye
1Ricerca Biosciences, 7528 Auburn Road, Concord, OH 44077, USA. reddy_l@ricerca.com
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.

