345207-40-1Relevant academic research and scientific papers
Synthesis and evaluation of N-((1-benzyl-1H-1,2,3-triazol-4-yl)methyl) nicotinamides as potential anticancer agents that inhibit tubulin polymerization
Kamal, Ahmed,Reddy, N.V. Subba,Nayak, V. Lakshma,Bolla, Narasimha Rao,Subba Rao,Prasad
, p. 3465 - 3477 (2014)
A series of N-((1-benzyl-1H-1,2,3-triazol-4-yl)methyl)nicotinamides (4) was synthesized and tested for their anticancer activity against a panel of 60 human cancer cell lines. Some of the representative compounds such as 4a, 4b, 4f, 4g, 4i and 4t were selected for the five dose study and amongst them 4g and 4i displayed significant anticancer activity with GI50 values ranging from 0.25 to 8.34 and 1.42 to 5.86 μM, respectively. Cell cycle analysis revealed that these compounds induced cell cycle arrest at G2/M phase in MCF-7 cells. The most active compound in this series 4g also inhibited tubulin polymerization with IC50 value 1.93 μM superior to that of E7010. Moreover, assay to investigate the effect on caspase-9, Hoechst staining and DNA fragmentation analysis suggested that these compounds induced cell death by apoptosis. Docking experiments showed that they interact and bind efficiently with tubulin protein. Overall, the results demonstrate that N-((1-benzyl-1H-1,2, 3-triazol-4-yl)methyl)nicotinamide scaffold possess anticancer property by inhibiting the tubulin polymerization.
N-((1-BENZYL-1H-1,2,3-TRIAZOL-4-YL)METHYL)ARYLAMIDE COMPOUNDS AS POTENTIAL ANTICANCER AGENTS AND A PROCESS FOR THE PREPARATION THEREOF
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Paragraph 0104, (2015/06/24)
The present invention provides a compound of general formula 1, useful as potential anticancer agents against human cancer cell lines and process for the preparation thereof. R1=H, 4-F, 4-Cl, 4-Br, 4-OMe, 3-F, 2,4-diOMe, 2,5-diOMe, 3,5-diOMe, 3
