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 ...