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Kamal, A. and Ramesh, G. and Srinivas, O. and Ramulu, P. and Laxman, N. and Rehana, T. and Deepak, M. and Achary, M.S. and Nagarajaram, H.A. (2004) Design, synthesis, and evaluation of mixed imine–amine pyrrolobenzodiazepine dimers with efficient DNA binding affinity and potent cytotoxicity. Bioorganic & Medicinal Chemistry, 12 (20). pp. 5427-5436. ISSN 0968-0896

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Synthesis of mixed imine-amine pyrrolobenzodiazepine (PBD) dimers that are comprised of DC-81 and secondary amine (N10) of DC-81 subunits tethered to their C8 positions through alkanedioxy linkers (comprised of three and five carbons) is described. These noncross-linking unsymmetrical molecules exhibit significant DNA minor groove binding ability and one of them 5b linked through the pentanedioxy chain exhibits efficient DNA binding ability (DeltaTm=11.0 degrees C) when compared to naturally occurring DC-81, 1 (DeltaTm=0.7 degrees C). The imine-amine PBD dimers exhibit promising in vitro antitumor activity in a number of human cancer cell lines.

Item Type: Article
Depositing User: Dr P Divakar
Date Deposited: 02 Jul 2015 07:27
Last Modified: 02 Jul 2015 07:27
URI: http://cdfd.sciencecentral.in/id/eprint/219

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