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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Enhancement of Drug Cytotoxicity by Silicon Containing Groups

Author(s): Jose M. Padron, Osvaldo J. Donadel, Leticia G. Leon, Tomas Martin and Victor S. Martin

Volume 3 , Issue 1 , 2006

Page: [29 - 34] Pages: 6

DOI: 10.2174/157018006775240944

Price: $65


Enantiomerically pure (2R,3S)-disubstituted tetrahydropyrans with diverse functional groups were synthesized. These derivatives were used as a model to study the influence of the tert-butyl dimethyl silyl group in the anticancer activity. The in vitro cytotoxicity was evaluated against a panel of six human cancer cells from diverse origin (MCF7, T-47D, HeLa, SW1573, WiDr and A2780). The structure-activity relationship study shows the relevant role of the silyl protecting group in the enhancement of the observed cytotoxic activity.

Keywords: Silyl ethers, antitumor agents, structure-activity relationships, lipophilicity, drug design

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