Synthesis, antimalarial activity and cytotoxicity of 4-aminoquinoline-triazine conjugates

Bioorg Med Chem Lett. 2010 Jan 1;20(1):322-5. doi: 10.1016/j.bmcl.2009.10.106.

Sunny Manohar ¹, Shabana I Khan, Diwan S Rawat

Affiliations

Affiliation

1 Department of Chemistry, University of Delhi, Delhi 110 007, India.

PMID: 19910192 DOI: 10.1016/j.bmcl.2009.10.106

Abstract

A series of 4-aminoquinoline-triazine conjugates with different substitution pattern have been synthesized and evaluated for their in vitro antimalarial activity against chloroquine-sensitive and resistant strains of Plasmodium falciparum. Compounds 16, 19, 28 and 35 exhibited promising antimalarial activity against both strains of P. falciparum. Cytotoxicity of these compounds was tested against three cell lines. Several compounds did not show any cytotoxicity up to a high concentration (48microM), Others exhibited mild toxicities but selective index for antimalarial activity was high for most of these conjugates.

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