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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.
AuthorsAnna I Koutsourea, Manolis A Fousteris, Evagelia S Arsenou, Athanasios Papageorgiou, George N Pairas, Sotiris S Nikolaropoulos
JournalBioorganic & medicinal chemistry (Bioorg Med Chem) Vol. 16 Issue 9 Pg. 5207-15 (May 01 2008) ISSN: 1464-3391 [Electronic] England
PMID18353651 (Publication Type: Journal Article)
Chemical References
  • Antineoplastic Agents
  • Esters
  • Steroids
Topics
  • Alkylation
  • Animals
  • Antineoplastic Agents (administration & dosage, chemical synthesis, chemistry)
  • Disease Models, Animal
  • Dose-Response Relationship, Drug
  • Drug Design
  • Drug Screening Assays, Antitumor
  • Esters (administration & dosage, chemical synthesis, chemistry)
  • Female
  • Injections, Intraperitoneal
  • Leukemia L1210 (drug therapy)
  • Leukemia P388 (drug therapy)
  • Male
  • Mice
  • Mice, Inbred BALB C
  • Mice, Inbred DBA
  • Molecular Structure
  • Neoplasm Transplantation
  • Neoplasms, Experimental (drug therapy)
  • Stereoisomerism
  • Steroids (administration & dosage, chemical synthesis, chemistry)
  • Structure-Activity Relationship

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