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

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

  • Bioorg Med Chem Lett. 2009 May 15;19(10):2760-2. doi: 10.1016/j.bmcl.2009.03.115.
Rahul S Nandurdikar 1,  Anna E Maciag,  Michael L Citro,  Paul J Shami,  Larry K Keefer,  Joseph E Saavedra,  Harinath Chakrapani
Affiliations

Affiliation

  • 1 Chemistry Section, Laboratory of Comparative Carcinogenesis, National Cancer Institute at Frederick, MD 21702, USA.
PMID: 19364650 DOI: 10.1016/j.bmcl.2009.03.115
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.

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