Synthesis and evaluation of piperazine and homopiperazine analogues of JS-K,an anti-cancer lead compound |
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| Authors: | Rahul S Nandurdikar Anna E Maciag Michael L Citro Paul J Shami Larry K Keefer Joseph E Saavedra Harinath Chakrapani |
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| Institution: | 1. Chemistry Section, Laboratory of Comparative Carcinogenesis, National Cancer Institute at Frederick, Frederick, MD 21702, USA;2. Basic Sciences Program, SAIC-Frederick, National Cancer Institute at Frederick, Frederick, MD 21702, USA;3. Division of Oncology, Department of Internal Medicine, University of Utah, Salt Lake City, UT 84112, USA |
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| 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 O2-(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. |
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