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Synthesis and cytotoxic evaluation of novel paraconic acid analogs.

Abstract：

:A novel class of 2,3-tri- and tetrasubstituted γ-butyrolactones analogous to paraconic acids has been synthesized in one step using a straightforward three-component reaction among aryl bromides, dimethyl itaconate and carbonyl compounds. The in vitro cytotoxic activity of representative compounds has been evaluated against a panel of human cancer cell lines (KB, HCT116, MCF7, HL60). While most molecules exhibit a low to moderate background activity on both KB and HL60 cancer cell lines, one compound shows increased antiproliferative activities against both cell lines with IC(50) values in the 10(-7)-10(-6)mol/L range. An extended evaluation indicated that this compound also inhibits PC3, SK-OV3, MCF7R and HL60R cell growth in the same fashion.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Le Floch C,Le Gall E,Léonel E,Martens T,Cresteil T

doi

10.1016/j.bmcl.2011.09.092

subject

Has Abstract

pub_date

2011-12-01 00:00:00

pages

7054-8

issue

23

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(11)01336-9

journal_volume

21

pub_type

杂志文章

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