Synthesis of some cryptolepine analogues, assessment of their antimalarial and cytotoxic activities, and consideration of their antimalarial mode of action

…, HI Dodson, M Feiz-Haddad, H Kendrick…

文献索引：Onyeibor, Onyeka; Croft, Simon L.; Dodson, Hilary I.; Feiz-Haddad, Mohammad; Kendrick, Howard; Millington, Nicola J.; Parapini, Silvia; Phillips, Roger M.; Seville, Scott; Shnyder, Steven D.; Taramelli, Donatella; Wright, Colin W. Journal of Medicinal Chemistry, 2005 , vol. 48, # 7 p. 2701 - 2709

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被引用次数: 93

摘要

A series of analogues of cryptolepine (1) have been synthesized and evaluated for their in vitro antiplasmodial and cytotoxic properties. The IC50 values of several compounds (11a, 11k-m, 11o, 13) against Plasmodium falciparum (strain K1) were< 0.1 μM, 5-10-fold lower than that of 1 but their cytotoxicities were only 2-4 times greater than that of 1. Compounds with a halogen in the quinoline ring and a halogen or a nitro group in the indole ring have ...