623163-52-0Relevant articles and documents
Synthesis and MEK1 inhibitory activities of imido-substituted 2-chloro-1,4-naphthoquinones
Bakare, Oladapo,Ashendel, Curtis L.,Peng, Hairuo,Zalkow, Leon H.,Burgess, Edward M.
, p. 3165 - 3170 (2003)
Mitogen activated protein kinases are of interest as research tools and as therapeutic target for certain physiological disorders. In this study, we found 2-chloro-3-(N-succinimidyl)-1,4-naphthoquinone 6 to be a selective inhibitor of MEK1 with an IC50 of 0.38 μM. An open-chain homologue, 10, showed selective cytotoxicity against renal cancer in the NCI in vitro tumor screening. Structure-activity relationship study of eight compounds showed the cyclic imido-substituted chloro-1,4-naphthoquinone as more potent and selective MEK1 inhibitors than the open chain homologues. The imido-substituted chloro-1,4-naphthoquinones were synthesized in a straightforward fashion by refluxing 2-amino-3-chloro-1,4-naphthoquinone with the appropriate acid chloride or diacyl dichloride.
Method for inhibiting Trypanosoma cruzi
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Page/Page column 22, (2016/09/26)
Methods are provided to inhibit proliferation of Trypanosoma cruzi with imido-substituted 1,4-naphthoquinones, including novel compounds. Administering an imido-substituted 1,4-naphthoquinone can be used to provide prophylaxis or treatment to a patient in
Antitrypanosomal activities and cytotoxicity of some novel imidosubstituted 1,4-naphthoquinone derivatives
Khraiwesh, Mozna H.,Lee, Clarence M.,Brandy, Yakini,Akinboye, Emmanuel S.,Berhe, Solomon,Gittens, Genelle,Abbas, Muneer M.,Ampy, Franklin R.,Ashraf, Mohammad,Bakare, Oladapo
experimental part, p. 27 - 33 (2012/07/02)
The antitrypanosomal activities, cytotoxicity, and selectivity indices of eleven imido-substituted 1,4-naphthoquinone derivatives and nifurtimox have been studied. Compared to nifurtimox (IC50 = 10.67 μM), all the imido-naphthoquinone analogs (
