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Sterols as anticancer agents: synthesis of ring-B oxygenated steroids, cytotoxic profile, and comprehensive SAR analysis.

Abstract：

:The cytotoxicity of oxysterols was systematically studied in tumor and normal cells. Synthetic strategies to prepare this library included oxidations at ring B and a new method to yield 6β-hemiphthalates directly from Δ(5)-steroids. Most oxysterols were cytotoxic and showed selectivity toward cancer cells, LAMA-84 cells (leukemia) being particularly sensitive to 4, 8, 22, and 27 (IC(50) < 5.6 μM). The structural requirements to induce selective toxicity are discussed to shed light on the development of new anticancer drugs.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Carvalho JF,Silva MM,Moreira JN,Simões S,Sá e Melo ML

doi

10.1021/jm1007769

subject

Has Abstract

pub_date

2010-11-11 00:00:00

pages

7632-8

issue

21

eissn

0022-2623

issn

1520-4804

journal_volume

53

pub_type

杂志文章

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