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Cytostatic effect of homo-aza-steroidal esters in vivo and in vitro. Structure-activity relationships.
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1992
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Pharmaceutical SciencePharmaceutical ChemistryMolecular PharmacologyMedicinal ChemistryAnti-cancer AgentP388 LeukemiaSteroid MetabolismCytostatic EffectOxysterolBiochemistryStructure-activity RelationshipsStructure-activity RelationshipP 388PharmacologyNatural SciencesMedicineHomo-aza-steroidal EstersDerivative (Chemistry)Drug Discovery
The p-[N,N-bis (2-chloroethyl)amino]phenylacetate esters of 3 beta-hydroxy-N-methyl-17 alpha-aza-D-homo-5 alpha-androstan-17-one and 3 beta-hydroxy-17 alpha-aza-D-homo-5 alpha-androstane have been prepared and their antitumor activity evaluated against L1210 leukemia, P388 leukemia, Ehrlich ascites tumor (EAT) and Lewis Lung Carcinoma (LLC). The results are compared with those of the p-[N,N-bis (2-chloroethyl)amino]phenylacetate of 3 beta-hydroxy-17 alpha-aza-D-homo- 5 alpha-androstan-17-one. The above compounds were also tested in vitro against L1210, P 388, EAT and BHX cell cultures. All compounds were found to be active and their structure-activity relationship is discussed.