Chemical and Pharmaceutical Bulletin · 2000 · 16 citations · 1 references
PharmacyMedicinal ChemistryPharmacologyCancer PharmacologyChemotherapyStructure-activity RelationshipsCytotoxic ChemotherapyOncology PharmacologyQuantitative Structure-activity RelationshipsStructure-activity Relationship AnalysisAnticancer ActivityChemical Structure-activity RelationshipsIn Vivo StudiesIndole ChemistryIndole DerivativesPyrazole ChemistryStereochemical Structure - Activity RelationshipStructure-activity Relationship Modeling
The structure activity relationship (SAR) in the anti-cancer activities of pyrazolo[1,5-a]indole derivatives was investigated, and the following conclusions were obtained: 1) N(1)-quaternarization is essential for anti-cancer activity, 2) the size and polarity of the 2-substituent is crucial for in vitro activity which allows further investigation in an in vivo test, 3) the effect of the 4-substituent on the activity is minor compared with the other two factors.
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