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The tert-butyl dimethyl silyl group as an enhancer of drug cytotoxicity against human tumor cells.

Abstract：

:In this study, we synthesized a series of enantiomerically pure (2R,3S)-disubstituted tetrahydropyranes with diverse functional groups using known methodologies. In addition to the tert-butyl dimethyl silyl group, other common protecting groups for hydroxyl groups such as allyl, acetate, and benzoate were used to obtain appropriate derivatives. Pure compounds were evaluated in vitro against HL60 human leukemia cells and MCF7 human breast cancer cells. From the growth inhibition data a structure-activity relationship was obtained. Overall the results point to the relevant role of the tert-butyl dimethyl silyl group in the modulation of cytotoxic activity.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Donadel OJ,Martín T,Martín VS,Villar J,Padrón JM

doi

10.1016/j.bmcl.2005.05.126

subject

Has Abstract

pub_date

2005-08-01 00:00:00

pages

3536-9

issue

15

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(05)00737-7

journal_volume

15

pub_type

杂志文章

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