2. Academic Validation
  3. Synthesis, anticancer activity and mitochondrial mediated apoptosis inducing ability of 2,5-diaryloxadiazole-pyrrolobenzodiazepine conjugates

Synthesis, anticancer activity and mitochondrial mediated apoptosis inducing ability of 2,5-diaryloxadiazole-pyrrolobenzodiazepine conjugates

  • Bioorg Med Chem. 2010 Sep 15;18(18):6666-77. doi: 10.1016/j.bmc.2010.07.067.
Ahmed Kamal 1,  D Dastagiri,  M Janaki Ramaiah,  E Vijaya Bharathi,  J Surendranadha Reddy,  G Balakishan,  Pranjal Sarma,  S N C V L Pushpavalli,  Manika Pal-Bhadra,  Aarti Juvekar,  Subrata Sen,  Surekha Zingde
Affiliations

Affiliation

  • 1 Chemical Biology Laboratory, Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500 607, India. ahmedkamal@iict.res.in
PMID: 20732817 DOI: 10.1016/j.bmc.2010.07.067
Abstract

A series of 2,5-diaryloxadiazole linked pyrrolo[2,1-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 microM. 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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