aLaboratory of Medicinal Chemistry, School of Health Sciences, Department of Pharmacy, University of Patras, 26500 Rion-Patras, Greece
bLaboratory of Experimental Chemotherapy, Theagenion Anticancer Hospital, Thessalonica, Greece
Abstract:
The synthesis and the in vivo evaluation against leukemias P388 and L1210 of six new alkylating steroidal esters are described. The esteric derivatives incorporating the 17β-acetamido-B-lactamic steroidal skeleton exhibited increased antileukemic activity and lower toxicity, compared to the 17β-acetamido-7-keto analogs. Among the 17β-acetamido-B-lactamic steroidal esters, the most potent compound afforded four out of six cures in leukemia P388 and was measured to be almost non-toxic, producing significant low levels of toxicity.