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https://hdl.handle.net/10316/27241
Title: | 4β-[4′-(1-(Aryl)ureido)benzamide]podophyllotoxins as DNA topoisomerase I and IIα inhibitors and apoptosis inducing agents | Authors: | Kamal, Ahmed Suresh, Paidakula Ramaiah, M. Janaki Reddy, T. Srinivasa Kapavarapu, Ravi Kumar Rao, Bolla Narasimha Imthiajali, Syed Reddy, T. Lakshminarayan Pushpavalli, S. N. C. V. L. Shankaraiah, Nagula Pal-Bhadra, Manika |
Keywords: | Etoposide; Podophyllotoxin; Cell cycle; Cytotoxicity; Topoisomerase-IIα enzyme; Topoisomerase-I enzyme | Issue Date: | 1-Sep-2013 | Publisher: | Elsevier | Citation: | KAMAL, Ahmed [et. al] - 4β-[4′-(1-(Aryl)ureido)benzamide]podophyllotoxins as DNA topoisomerase I and IIα inhibitors and apoptosis inducing agents. "Bioorganic & Medicinal Chemistry". ISSN 0968-0896. Vol. 21 Nº. 17 (2013) p. 5198-5208 | Serial title, monograph or event: | Bioorganic & Medicinal Chemistry | Volume: | 21 | Issue: | 17 | Abstract: | A series of 4β-[4′-(1-(aryl)ureido)benzamide]podophyllotoxin congeners (11a–l) were synthesized and evaluated for their cytotoxic activity against six human cancer cell lines. Some of the compounds like 11a, 11h, 11k and 11l showed significant anti-proliferative activity in Colo-205 cells and were superior to etoposide. The flow-cytometric analysis studies indicated that these compounds show strong G1 cell cycle arrest, as well exhibited improved inhibitory activities on DNA topoisomerase I and IIα enzymes. These compounds induce apoptosis by up regulating caspase-3 protein as observed by ELISA and Western blotting analysis. In addition, a brief structure–activity relationship studies within the series along with docking results of representative compounds 11a, 11h, 11k, 11l were presented. | URI: | https://hdl.handle.net/10316/27241 | ISSN: | 0968-0896 | DOI: | 10.1016/j.bmc.2013.06.033 | Rights: | openAccess |
Appears in Collections: | I&D CNC - Artigos em Revistas Internacionais |
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4β-[4’-(1-(Aryl)ureido)benzamide]podophyllotoxins.pdf | 1.42 MB | Adobe PDF | View/Open |
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