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Hederagenin as a triterpene template for the development of new antitumor compounds.

Abstract：

:In this study, a series of novel C-28 esters and amides derivatives of hederagenin (He) were designed and synthesized in attempt to develop potent antitumor agents. Their structures were confirmed by MS, IR, (1)H NMR and (13)C NMR spectroscopic analyses and their cytotoxic activities were screened in SRB assays using a panel of six human cancer cell lines. Although most of the compounds displayed moderate to high levels of cytotoxic activity they were all more potent than the natural product He. The most active compounds had either an ethylpyrimidinyl (27) or an ethylpyrrolidinyl (28) substituent, with EC50 in the range of 1.1-6.5 μM for six human cancer cell lines. Notably, this corresponds to an approximately 30-fold times greater potency than He.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Rodríguez-Hernández D,Demuner AJ,Barbosa LC,Csuk R,Heller L

doi

10.1016/j.ejmech.2015.10.006

subject

Has Abstract

pub_date

2015-11-13 00:00:00

pages

57-62

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(15)30288-9

journal_volume

105

pub_type

杂志文章

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