Antileukemic compounds derived from the chemical modification of macrocyclic trichothecenes. 1. Derivatives of verrucarin A

BB Jarvis, GP Stahly, G Pavanasasivam…

Index: Jarvis, Bruce B.; Stahly, G. Patrick; Pavanasasivam, Gowsala; Mazzola, Eugene P. Journal of Medicinal Chemistry, 1980 , vol. 23, # 9 p. 1054 - 1058

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Citation Number: 48

Abstract

Verrucarin A (2) was epoxidized to give the 0-9, lO-epoxide 7 (major product) and a-9, lO- epoxide 9 (minor product). The 0-epoxide 7 and its acetate 8 exhibit high in vivo antileukemic activity against P-388 mouse leukemia, whereas 2 and 9 are inactive. Epoxidation of verrucarin B (3) and roridin A (1) to their respective 0-9, lO-epoxides (11 and 12, respectively) also yields compounds with substantially increased activity. Allylic ...