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U.S. Department of Health and Human Services

Scientific Publications by FDA Staff

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J Pharm Sci 1982 May;71(5):542-51

Synthesis, hydrolytic reactivity, and anticancer evaluation of N- and O-triorganosilylated compounds as new types of potential prodrugs.

Chiu FT, Chang YH, Ozkan G, Zon G, Fichter KC, Phillips LR


N- and O-Triorganosilylated compounds related to various anticancer agents were synthesized for evaluation as potential anticancer prodrugs. 1H-NMR and UV kinetic measurements of hydrolytic desilylation were used to correlate relative rates of structural unmasking with steric bulk about the silicon reaction center. The tert-butyldimethylsilyl ester of chlorambucil and a number of O- triorganosilylated carbamate derivatives of nor-nitrogen mustard showed significant activity against P-388 lymphocytic leukemia in mice.

Category: Journal Article
PubMed ID: #7097502 DOI: 10.1002/jps.2600710517
Includes FDA Authors from Scientific Area(s): Biologics
Entry Created: 2012-12-09