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.
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Authors | Anna I Koutsourea, Manolis A Fousteris, Evagelia S Arsenou, Athanasios Papageorgiou, George N Pairas, Sotiris S Nikolaropoulos |
Journal | Bioorganic & medicinal chemistry
(Bioorg Med Chem)
Vol. 16
Issue 9
Pg. 5207-15
(May 01 2008)
ISSN: 1464-3391 [Electronic] England |
PMID | 18353651
(Publication Type: Journal Article)
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Chemical References |
- Antineoplastic Agents
- Esters
- Steroids
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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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