| Literature DB >> 20557981 |
Ahmed Kamal1, J Surendranadha Reddy, M Janaki Ramaiah, D Dastagiri, E Vijaya Bharathi, M Ameruddin Azhar, Farheen Sultana, S N C V L Pushpavalli, Manika Pal-Bhadra, Aarti Juvekar, Subrata Sen, Surekha Zingde.
Abstract
A series of 3,5-diaryl-isoxazoline/isoxazole linked pyrrolo[2,1-c][1,4]benzodiazepine (PBD) conjugates were prepared. These conjugates showed potent anticancer activity with GI(50) values in the range of <0.1-3.6 microM. Some of these PBD conjugates (6a-c) with promising anticancer activity were further investigated on the cell cycle distribution. Moreover, these PBD conjugates exhibited G0/G1 arrest, enhancement in the levels of p53 protein as well as mitochondrial-mediated intrinsic pathway, leading to release of cytochrome c, activation of caspase-3, cleavage of PARP and subsequent apoptotic cell death. Hence these PBD conjugates with 6a being the most potent one could be be taken up for preclinical studies either alone or in combination with existing therapies. 2010 Elsevier Masson SAS. All rights reserved.Entities:
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Year: 2010 PMID： 20557981 DOI： 10.1016/j.ejmech.2010.05.047
Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514