title: Rational design, synthesis, and in vivo evaluation of the antileukemic activity of six new alkylating steroidal esters.
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 17beta-acetamido-B-lactamic steroidal skeleton exhibited increased antileukemic activity and lower toxicity, compared to the 17beta-acetamido-7-keto analogs. Among the 17beta-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.
authors: Laboratory of Medicinal Chemistry, School of Health Sciences, Department of Pharmacy, University of Patras, 26500 Rion-Patras, Greece.
authors: Anna I
authors: AI
authors: Koutsourea
authors: Manolis A
authors: MA
authors: Fousteris
authors: Evagelia S
authors: ES
authors: Arsenou
authors: Athanasios
authors: A
authors: Papageorgiou
authors: George N
authors: GN
authors: Pairas
authors: Sotiris S
authors: SS
authors: Nikolaropoulos
mesh_terms: D000478:Alkylation; D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage / Q000138:chemical synthesis / Q000737:chemistry; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D004952:Esters / Q000008:administration & dosage / Q000138:chemical synthesis / Q000737:chemistry; D005260:Female; D007274:Injections, Intraperitoneal; D007939:Leukemia L1210 / Q000188:drug therapy*; D007941:Leukemia P388 / Q000188:drug therapy*; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D008811:Mice, Inbred DBA; D015394:Molecular Structure; D009368:Neoplasm Transplantation; D009374:Neoplasms, Experimental / Q000188:drug therapy; D013237:Stereoisomerism; D013256:Steroids / Q000008:administration & dosage / Q000138:chemical synthesis / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: D000970:Antineoplastic Agents; D004952:Esters; D013256:Steroids