期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 114, 期 -, 页码 220-231出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2016.02.059
关键词
Pyrrolo[2,3-b]pyridine; 1,2,3-Triazole; Calf thymus DNA; Antiproliferative activity
资金
- Department of Biotechnology (DBT), Government of India, New Delhi [BT/PR4801/MED/29/370/2012]
- UGC, New Delhi
A series of thirty two novel pyrrolo[2,3-b]pyridine analogues synthesized, characterized (H-1 NMR, C-13 NMR and MS) and cytotoxic evaluation of these molecules carried out over a panel of three human cancer cell lines including A549 (lung cancer), HeLa (cervical cancer) and MDA MB-231 (breast cancer), using sulforhodamine B assay method. Few molecules such as 5c, 5d, 5e, 5h, 5k, 5m, 5n, 5q, 5r, 7f, 7j, 7g and 7k exhibited maximum growth inhibitory action against the tested cancer cell lines at lower micro molar concentration. Noticeably, compounds exhibited good growth inhibition in all three cancer cell lines in the range of 0.12 mu M-9.84 mu M. Further study exposed that one of the active compound 5d could efficiently intercalate into calf thymus DNA to form 5d-DNA complex which might block DNA replication to influence their antiproliferative activity. The molecular interactions of all the synthesized analogs were also supported by molecular docking simulations. We believe that further optimization of these compounds will lead to potential anticancer agents. (C) 2016 Elsevier Masson SAS. All rights reserved.
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