- Synthesis, antitumor evaluation, and molecular docking studies of indole–indazolyl hydrazide–hydrazone derivatives
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Abstract: A series of ten novel hydrazide–hydrazones linked indole and indazole moieties were designed and synthesized. All the synthesized compounds were evaluated for their cytotoxicity against four human cancer cell lines (HeLa, MDA-MB-231, MCF-7, and A549). Three of the synthesized compounds showed promising cytotoxicity specifically on some of the tested cell lines with IC50 values ranging between 1.93 and 25.6?μM. Further, one compound was identified as a promising drug lead which showed promising cytotoxicity with IC50 value of 1.93?μM towards MCF-7 breast cancer cell line as compared to the standard drug doxorubicin (IC50 value 0.98?μM). While, all these new compounds showed no cytotoxicity on the normal human embryonic kidney cell line, HEK-293. Graphical abstract: [Figure not available: see fulltext.]
- Sreenivasulu, Reddymasu,Sujitha, Pombala,Jadav, Surender Singh,Ahsan, Mohamed Jawed,Kumar, C. Ganesh,Raju, Rudraraju Ramesh
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- An optimized procedure for direct access to 1: H -indazole-3-carboxaldehyde derivatives by nitrosation of indoles
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Indazole derivatives are currently drawing more and more attention in medicinal chemistry as kinase inhibitors. 1H-indazole-3-carboxaldehydes are key intermediates to access to a variety of polyfunctionalized 3-substituted indazoles. We report here a general access to this motif, based on the nitrosation of indoles in a slightly acidic environment. These very mild conditions allow the conversion of both electron-rich and electron-deficient indoles into 1H-indazole-3-carboxaldehydes.
- Chevalier, Arnaud,Ouahrouch, Abdelaaziz,Arnaud, Alexandre,Gallavardin, Thibault,Franck, Xavier
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p. 13121 - 13128
(2018/04/23)
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- Synthesis and anticancer evaluation of indazole-aryl hydrazide-hydrazone derivatives
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A new series of hydrazide-hydrazones linked between indazole and substituted benzaldehydes were designed, synthesized and evaluated for their cytotoxicity against four human cancer cell lines (HeLa, MDA-MB-231, MCF-7 and A549). Among the synthesized compo
- Rudavath, Durgesh,Sreenivasulu, Reddymasu,Pinapati, Srinivasa Rao,Raju, Rudraraju Ramesh
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p. 433 - 438
(2020/06/29)
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- Indazolecarboxamide derivatives, preparation and use thereof as CDK1, CDK2 and CDK4 inhibitors
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Compound corresponding to general formula (I): [image] in which, R1 represents a hydrogen or halogen atom, an NH2, NHR2, NHCOR2, NO2, CN, CH2NH2 and CH2NHR2; or alternatively R1 represents an optionally substituted phenyl or an optionally substituted heteroaromatic group; Ar represents an optionally substituted phenyl group or an optionally substituted heteroaromatic group; n represents 0, 1, 2 or 3; in the form of a base, of an addition salt with an acid, of a hydrate or of a solvate. Application in therapy.
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Page/Page column 17
(2008/06/13)
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