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Synthesis and evaluation of piperazine and homopiperazine analogues of JS-K, an anti-cancer lead compound.

Abstract：

:Here we report a number of novel JS-K structural analogues with sub-micromolar anti-proliferative activities against human leukemia cell lines HL-60 and U937; JS-K is the anti-cancer lead compound O(2)-(2,4-dinitrophenyl) 1-[(4-ethoxycarbonyl)piperazin-1-yl]diazen-1-ium-1,2-diolate. The ability of these compounds to generate intracellular nitric oxide correlated well with their observed anti-proliferative effects: analogues that had potent inhibitory activity against leukemia cells formed elevated levels of intracellular nitric oxide.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Nandurdikar RS,Maciag AE,Citro ML,Shami PJ,Keefer LK,Saavedra JE,Chakrapani H

doi

10.1016/j.bmcl.2009.03.115

subject

Has Abstract

pub_date

2009-05-15 00:00:00

pages

2760-2

issue

10

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(09)00442-9

journal_volume

19

pub_type

杂志文章

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