Facile synthesis of 1,2,3-triazole-fused indolo- and pyrrolo[1,4]diazepines, DNA-binding and evaluation of their anticancer activity.

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ID: 57919
2019
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Abstract
A facile synthetic strategy has been developed for the generation of structurally diverse N-fused heterocycles. The formation of fused 1,2,3-triazole indolo and pyrrolodiazepines proceeds through an initial Knoevenagel condensation followed by intramolecular azide-alkyne cycloaddition reaction at room temperature without recourse to the traditional Cu(I)-catalyzed azide-alkyne cycloadditions. The synthesized compounds were evaluated for their in vitro anti-cancer activity against the NCI 60 cell line panel. Among the tested compounds, 3a and 3h were found to exhibit potent inhibitory activity against many of the cell lines. Cell cycle analysis indicated that the compounds inhibit the cell cycle at sub G1 phase. The DNA- nano drop method, viscosity experiment and docking studies suggested these compounds possess DNA binding affinity.
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gour2019facilebioorganic Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Gour, Jitendra;Gatadi, Srikanth;Pooladanda, Venkatesh;Ghouse, Shaik Mahammad;Malasala, Satyaveni;Madhavi, Y V;Godugu, Chandraiah;Nanduri, Srinivas;
Journal Bioorganic chemistry
Year 2019
DOI
S0045-2068(19)31025-9
URL
Keywords
Cytotoxicity dna-binding fused polycyclics mda-mb-468 cancer cells

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