Synthesis, hydrolytic reactivity, and anticancer evaluation of N??and 0??triorganosilylated compounds as new types of potential prodrugs

…, YH Chang, G Özkan, G Zon, KC Fichter…

Index: Chiu; Chang; Ozkan; Zon; Fichter; Phillips Journal of Pharmaceutical Sciences, 1982 , vol. 71, # 5 p. 542 - 551

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Citation Number: 17

Abstract

Abstract N-and O-Triorganosilylated compounds related to various anticancer agents were synthesized for evaluation as potential anticancer prodrugs. 1 H-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- ...