Cytotoxic Activity of Styryl Lactones and their Derivatives

ISSN: 1875-5992 (Online)
ISSN: 1871-5206 (Print)

Volume 17, 14 Issues, 2017

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Anti-Cancer Agents in Medicinal Chemistry

Formerly: Current Medicinal Chemistry - Anti-Cancer Agents

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  • 27th of 59 in Chemistry, Medicinal

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Michelle Prudhomme
Institut de Chimie de Clermont-Ferrand
Université Clermont Auvergne

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Cytotoxic Activity of Styryl Lactones and their Derivatives

Anti-Cancer Agents in Medicinal Chemistry, 1(3): 293-300.

Author(s): Hari Babu Mereyala and Maju Joe.

Affiliation: Organic Chemistry Division III, Fine Chemical Laboratory, Indian Institute of Chemical Technology, Hyderabad 500 007, India.


Many studies that have been conducted to establish the cytotoxic potency of styryl lactones for several tumor cell lines is described. Extensive examination of the activity of more than 50 cytotoxic styryl lactones isolated/synthesized belonging to the genus goniothalamus representing future generation of antitumor drugs is described for the first time at the molecular level. Goniopypyrone (39) is the most cytotoxic compound followed by altholactone (+)-1 (10-5 to 10-7 molar for IC50). Enantiomer (-)-1 and three stereocongeners 2-4 did not exhibit any significant increase in cytotoxicity. Cytotoxicity of semisynthetically derived products 5-11 is discussed recognising 11-nitro altho-lactone (+)-5 as a promising lead compound. Eight membered styryl lactones 12a - 12e are substrates with important cytotoxicity explained by the inhibition of the mammalian mitochondrial respiratory chain complex I. Among C7-C8 functionalised styryl lactones gonio diol (25) is the most active being selectively cytotoxic against A549 tumour cells. Goniofufurone (42) and several of its derivatives including one carbon homologues 43-50 were reported to be inactive.

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Article Details

Volume: 1
Issue Number: 3
First Page: 293
Last Page: 300
Page Count: 8
DOI: 10.2174/1568011013354606
Price: $58

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