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Issue 103, 2016
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Synthesis and biological evaluation of sapinofuranones A,B and 1,2,3-triazole-sapinofuranone hybrids as cytotoxic agents

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Abstract

The total synthesis of sapinofuranones A,B and ent-sapinofuranones A,B and L-factor has been described. A series of novel 1,2,3-triazole-sapinofuranone hybrids were efficiently synthesized employing a click chemistry approach. These sapinofuranones and 1,2,3-triazole-sapinofuranone hybrids were further evaluated for their cytotoxic activity against four human cancer cell lines (A549, MDA-MB-231, DU145 and HepG2). Most of them revealed cytotoxic effects against cancer cells at the micromolar range. From a structure–activity relationship (SAR) perspective, it was noticed that the combination of triazole moiety to the lactone ring is playing modest role in exhibiting the cytotoxic effect. This is the first report on the synthesis and in vitro cytotoxic evaluation of 1,2,3-triazole-sapinofuranone hybrids.

Graphical abstract: Synthesis and biological evaluation of sapinofuranones A,B and 1,2,3-triazole-sapinofuranone hybrids as cytotoxic agents

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Publication details

The article was received on 01 Sep 2016, accepted on 08 Oct 2016 and first published on 14 Oct 2016


Article type: Communication
DOI: 10.1039/C6RA21939J
Citation: RSC Adv., 2016,6, 101501-101512
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    Synthesis and biological evaluation of sapinofuranones A,B and 1,2,3-triazole-sapinofuranone hybrids as cytotoxic agents

    K. S. Nagi Reddy, G. Sabitha, Y. Poornachandra and C. G. Kumar, RSC Adv., 2016, 6, 101501
    DOI: 10.1039/C6RA21939J

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