Structure–activity relationship of antiparasitic and cytotoxic indoloquinoline alkaloids, and their tricyclic and bicyclic analogues

Gitte Van Baelen,Steven Hostyn,Liene Dhooghe,Pál Tapolcsányi,Péter Mátyus,Guy Lemière,Roger Dommisse,Marcel Kaiser,Reto Brun,Paul Cos,Louis Maes,György Hajós,Zsuzsanna Riedl,Ildikó Nagy,Bert U.W. Maes,Luc Pieters

Bioorganic & Medicinal Chemistry（2009）

Cited 82|Views12

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Abstract

In a series of carbolines, azaindoles and pyrrolo(iso)quinolines, 2-methyl-β-carboline (9) showed the highest in vitro activity (IC50=0.45μM) against Plasmodium falciparum K1, without apparent cytotoxicity against L6 cells (SI>1000).

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Key words

Indoloquinoline alkaloid,Indoloisoquinoline,Carboline,Azaindole,Pyrroloquinoline,Pyrroloisoquinoline,Antiparasitic,Antiplasmodial,Antimalarial,Cytotoxic

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