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2-[(Carboxymethyl)sulfanyl]-4-oxo-4-arylbutanoic acids selectively suppressed proliferation of neoplastic human HeLa cells. A SAR/QSAR study.

Abstract：

:A series of twenty alkyl-, halo-, and methoxy-aryl-substituted 2-[(carboxymethyl)sulfanyl]-4-oxo-4-arylbutanoic acids were synthesized. The new compounds, called CSAB, suppressed proliferation of human cervix carcinoma, HeLa cells, in vitro in a concentration range of 0.644 to 29.48 microM/L. Two compounds exhibit antiproliferative activity in sub-micromolar concentrations. Five compounds act in low micromolar concentrations (<2 microM/L). The most active compounds exert lower cytotoxicity toward healthy human peripheral blood mononuclear cells (PBMC and PBMC+PHA) (selectivity indexes > 10). A strong structure-activity relationship, using estimated log P values and BCUT descriptors, was observed.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Drakulić BJ,Juranić ZD,Stanojković TP,Juranić IO

doi

10.1021/jm0502889

keywords:

subject

Has Abstract

pub_date

2005-08-25 00:00:00

pages

5600-3

issue

17

eissn

0022-2623

issn

1520-4804

journal_volume

48

pub_type

杂志文章

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