Synthesis and antitumor evaluation of methyl spongoate analogs.

Abstract:

:A series of novel methyl spongoate (1) analogs has been synthesized and evaluated for their in vitro cytotoxic properties. It was found that the nature of the C-20 side chain had significant effects on their bioactivities and some analogs showed higher cytotoxicity than 1 against A549, HCT-116, HepG2, SW-1990, MCF-7 and NCI-H460 tumor cell lines. The pharmacological results confirmed that the α,β-unsaturated carbonyl moiety, a Michael acceptor in ring A, plays a pivotal role in the cytotoxic effect of these derivatives. The compiled pharmacological data may be useful for the design of novel analogous anticancer drugs.

journal_name

Steroids

journal_title

Steroids

authors

Jiang CS,Huang CG,Feng B,Li J,Gong JX,Kurtán T,Guo YW

doi

10.1016/j.steroids.2010.08.002

subject

Has Abstract

pub_date

2010-12-12 00:00:00

pages

1153-63

issue

13-14

eissn

0039-128X

issn

1878-5867

pii

S0039-128X(10)00223-0

journal_volume

75

pub_type

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