Publication | Open Access
Antitumor Agents. V. Synthesis and Antileukemic Activity of E-Ring-Modified (RS)-Camptothecin Analogues.
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1992
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Chemoprevention StrategyPharmacotherapyPharmaceutical ChemistryMedicinal ChemistryAntitumor AgentsAnti-cancer AgentRadiation OncologyFriedländer CondensationPharmacological AgentTotal SynthesisV. SynthesisDrug DevelopmentSeveral E-ring-modified AnaloguesNatural Product SynthesisPharmacology-Camptothecin AnaloguesMedicineSynthetic ChemistryDrug Discovery
Several E-ring-modified analogues of (RS)-camptothecin were synthesized by total synthesis via Friedländer condensation and evaluated for cytotoxicity and antitumor activity against P388 mouse leukemia cells. Among them, (RS)-20-deoxyamino-7-ethyl-10-methoxycamptothecin (25c) was found to be more active than (RS)-camptothecin (1) in the in vivo assay.