Synthesis and biological evaluation of novel 4-(hetero) aryl-2-piperazino quinazolines as anti-leishmanial and anti-proliferative agents

Bioorg Med Chem Lett. 2009 May 1;19(9):2542-5. doi: 10.1016/j.bmcl.2009.03.020.

Shailesh Kumar ¹, Nishi Shakya, Suman Gupta, Jayanta Sarkar, Devi Prasad Sahu

Affiliations

Affiliation

1 Division of Medicinal Chemistry, Central Drug Research Institute, Lucknow, India.

PMID: 19328690 DOI: 10.1016/j.bmcl.2009.03.020

Abstract

A series of new class of 4-(hetero)aryl-2-piperazino quinazolines were synthesized and assessed for in vitro activity against extracellular promastigotes and intracellular amastigotes of Leishmania donovani. Among the compounds evaluated, compound 4bb and 4cb showed the selectivity index (SI) value>8.03 and 4.21, respectively, which is promising as compared with sodium stilbogluconate (SSG) and pentamidine with the SI of 6.38 and 2.07, respectively. The synthesized compounds were also tested for anti-proliferation activity in a panel of mammalian cell lines. Compound 4aa which is quite inactive and 4ab which is hardly selective in anti-leishmanial assay are found to have significant activity in anti-proliferative assay.

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