Cardiac glycosides. 6. Gitoxigenin C16 acetates, formates, methoxycarbonates, and digitoxosides. Synthesis and Na+, K+-ATPase inhibitory activities

T Hashimoto, H Rathore, D Satoh…

Index: Hashimoto, Toshihiro; Rathore, Hargovind; Satoh, Daisuke; Hong, George; Griffin, Jane F.; et al. Journal of Medicinal Chemistry, 1986 , vol. 29, # 6 p. 997 - 1003

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Citation Number: 19

Abstract

A series of 17 gitoxigenin 16p-formates, acetates, and methoxycarbonates was synthesized, including their 30-acetates, formates, and digitoxosides. A 160-formate group was generally found to increase activity 30 times, a 160-acetate group 9-12 times, while a 160- methoxycarbonate decreased activity by two-thirds. 30-Formates and acetates had little effect on activity by themselves, but sometimes reduced the activity-increasing properties ...