Department of Chemistry
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Item β‐Polynitration of 5,10,15,20‐tetrakis(2′,6′‐Dichlorophenyl)porphyrins with HNO3 and Cu(NO3)2 on Clay Using Microwave Irradiation(Taylor & Francis, 2004) Kumar, AnilAn expeditious β‐polynitration of 5,10,15,20‐tetrakis(2′,6′‐dichlorophenyl)porphyrin, its Zn and Cu derivatives with montmorillonite K10‐HNO3 and montmorillonite K10‐Cu(NO3)2 (claycop) under mild conditions using microwave irradiation in 72–95% yields has been described.Item Ionic liquid catalyzed expeditious synthesis of 2-aryl-2,3-dihydroquinolin-4(1H)-ones and 2-aryl-2,3-dihydro-4H-chromen-4-ones under microwave irradiation(Wiley, 2009-06-19) Kumar, Anil; Kumar, DalipA facile and convenient synthesis of 2-aryl-2,3-dihydroquinolin-4(1H)-one and 2-aryl-2,3-dihydro-4H-chromen-4-one has been described using ionic liquid catalyzed intramolecular cyclization of the corresponding 2′-aminochalcones and 2′-hydroxychalcones, respectively. The rapid and fairly general protocol affords product in good yield. Ionic liquid, 1-butyl-3-methylimidazolium tetrafluoroborate, was recovered and reused without loosing its efficiencyItem A Facile and Microwave-assisted Rapid Synthesis of 2-Arylamino-4-(3'-indolyl)- thiazoles as Apoptosis Inducing Cytotoxic Agents(Bentham Science, 2017) Kumar, Anil; Kumar, DalipThe clinical success of the chemotherapeutic drugs is restricted by the nonspecific toxicity-related adverse side effects. The diverse implication of indoles and thiazoles in medicinal chemistry prompted us to develop a new series of novel 2-aryl-amino-4-(3′-indolyl)thiazoles as more effective and less toxic anti-cancer compounds. Method and Results: One-pot microwave-assisted rapid and high yielding synthesis of 2-arylamino-4-(3′- indolyl)thiazoles involved the reaction of easily available α-tosyloxy-ketones with N-arylthioureas in polyethylene glycol-400 (PEG-400). In vitro cytotoxicity study of 2-arylamino-4-(3′-indolyl)thiazoles against a panel of human cancer cell lines by MTT assay revealed IC50 values in the low micromolar range. Of the fifteen synthesized arylaminothiazoles, compounds 17b, 17d, 17g and 17il showed significant anti-proliferative activity against the selected cancer cell lines with IC50 < 10 μM. The compound 17b was identified as the most potent ligand of the series, which exhibited good cytotoxic activity against MCF-7 breast cancer cells with an IC50 value of 1.86 μM but minimal toxicity on normal human cells. Investigation of the underlying mechanism by flow cytometry indicated that 17b induced ROS-mediated apoptosis in MCF-7 cells in a dose-dependent manner as supported by upregulation of Bax and caspase-3 and down-regulation of Bcl-2 (by Western blot).