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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.
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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