BITS Faculty Publications
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Item Click chemistry inspired synthesis of piperazine-triazole derivatives and evaluation of their antimicrobial activities(Springer, 2015) Jha, Prabhat N.; Kumar, AnilA series of novel piperazine-1,2,3-triazole derivatives, which entailed the bioisosteric replacement of the imidazole moiety and hybridization of two drug scaffolds was prepared by employing the regioselective copper (I)-catalysed azide-alkyne 1,3-dipolar cycloaddition reaction. The synthesized compounds were evaluated for antibacterial activities against Gram-negative (E. Coli and P. Putida), Gram-positive S. Aureus bacteria and fungicidal activities against F. oxysporum, F. gramillarium and F. monalliforme fungi. Compound 7ac′ exhibited moderate but promising antibacterial activity against Gram-negative bacteria and fungicidal activity against F. oxysporum and F. gramillarium.Item A Facile Synthesis and Cytotoxicity of a Novel Porphyrin-Cryptolepine Conjugate(CBI, 2012) Kumar, Anil; Kumar, DalipA novel porphyrin–cryptolepine conjugate 7 with a 1,2,3-triazole linker was synthesized by the cycloaddition reaction of propargyl porphyrin 2 and azido cryptolepine 6 under click conditions. The conjugate 7 exhibited enhanced photocytotoxicity against A549 cells with IC50 values of 2.5 μM and 7.9 μM in the visible and UV light, respectively.Item Synthesis of 3-phenylpyrazolopyrimidine-1,2,3-triazole conjugates and evaluation of their Src kinase inhibitory and anticancer activities(Elsiever, 2011-03) Kumar, AnilA series of two classes of 3-phenylpyrazolopyrimidine-1,2,3-triazole conjugates were synthesized using click chemistry approach. All compounds were evaluated for inhibition of Src kinase and human ovarian adenocarcinoma (SK-Ov-3), breast carcinoma (MDA-MB-361), and colon adenocarcinoma (HT-29). Hexyl triazolyl-substituted 3-phenylpyrazolopyrimidine exhibited inhibition of Src kinase with an IC50 value of 5.6 μM. 4-Methoxyphenyl triazolyl-substituted 3-phenylpyrazolopyrimidine inhibited the cell proliferation of HT-29 and SK-Ov-3 by 73% and 58%, respectively, at a concentration of 50 μM.