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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Kumar S,Shakya N,Gupta S,Sarkar J,Sahu DP

doi

10.1016/j.bmcl.2009.03.020

subject

Has Abstract

pub_date

2009-05-01 00:00:00

pages

2542-5

issue

9

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(09)00338-2

journal_volume

19

pub_type

杂志文章

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