Synthesis,anticancer activity and mitochondrial mediated apoptosis inducing ability of 2,5-diaryloxadiazole–pyrrolobenzodiazepine conjugates |
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Authors: | Ahmed Kamal D Dastagiri M Janaki Ramaiah E Vijaya Bharathi J Surendranadha Reddy G Balakishan Pranjal Sarma SNCVL Pushpavalli Manika Pal-Bhadra Aarti Juvekar Subrata Sen Surekha Zingde |
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Institution: | 1. Chemical Biology Laboratory, Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500 607, India;2. Advanced Centre for Treatment, Research & Education in Cancer, Navi Mumbai 400 611, India |
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Abstract: | A series of 2,5-diaryloxadiazole linked pyrrolo2,1-c]1,4]benzodiazepine conjugates have been prepared and evaluated for their anticancer activity. These conjugates have shown promising activity with GI50 values ranging from <0.1 to 0.29 μΜ. It is observed that some of these conjugates particularly 4a, 4d, 4i and 4l exhibit significant anticancer activity. Some detailed biological assays relating to the cell cycle aspects associated to Bax and caspases have been examined with a view to understand the mechanism of action of these conjugates. |
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