Synthesis, anticancer activity and apoptosis inducing ability of anthranilamide-PBD conjugates

• Published in: Bioorganic & medicinal chemistry letters Vol. 20; no. 11; pp. 3310 - 3313
• Main Authors: Kamal, Ahmed, Vijaya Bharathi, E., Janaki Ramaiah, M., Surendranadha Reddy, J., Dastagiri, D., Viswanath, A., Sultana, Farheen, Pushpavalli, S.N.C.V.L., Pal-Bhadra, Manika, Juvekar, Aarti, Sen, Subrata, Zingde, Surekha
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 01-06-2010
• Subjects: Active caspase-3; Anthranilamide; Anticancer activity; Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - pharmacology; Apoptosis; Benzodiazepines - chemistry; Caspase 3 - metabolism; Cell Cycle - drug effects; Cell Line, Tumor; Flow Cytometry; Humans; ortho-Aminobenzoates - chemical synthesis; ortho-Aminobenzoates - chemistry; ortho-Aminobenzoates - pharmacology; p53; Pyrroles - chemistry; Pyrrolobenzodiazepine; Tumor Suppressor Protein p53 - metabolism; Active caspase-3; Anthranilamide; Pyrrolobenzodiazepine; Anticancer activity; Apoptosis; p53
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/j.bmcl.2010.04.037

A series of novel anthranilamide linked pyrrolo[2,1-c][1,4]benzodiazepine conjugates were prepared and evaluated for their anticancer activity. The effects of three promising PBD conjugates on cell cycle of cancerous cell line A375 were investigated. These promising compounds showed the characteristic features of apoptosis like enhancement in the levels of p53 and activation of caspase-3.