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Medicinal Chemistry


ISSN (Print): 1573-4064
ISSN (Online): 1875-6638

Synthesis, DNA Binding Ability and Anticancer Activity of 2-heteroaryl Substituted Benzimidazoles Linked Pyrrolo[2,1-c][1,4]benzodiazepine Conjugates

Author(s): Ahmed Kamal, Praveen Kumar Pogula, Mohammed Naseer Ahmed Khan, Bobburi Naga Seshadri and Kokkonda Sreekanth

Volume 9 , Issue 5 , 2013

Page: [651 - 659] Pages: 9

DOI: 10.2174/1573406411309050004

Price: $65


As a continuation of our efforts to develop the benzimidazole-PBD conjugates as potential anticancer agents, a series of heteroaryl substituted benzimidazole linked PBD conjugates has been synthesized and evaluated for their anticancer potential in 60 human cancer cell lines. Most of the compounds exhibited promising anticancer activity and interestingly, compounds 4c and 4d displayed significant activity in most of the cell lines tested. Whereas, compound 4e showed selectivity in renal cancer cells with GI50 values of < 10 and 70 nM against RXF 393 and UO-31 cell lines, respectively. Further, these compounds also showed significant DNA-binding affinity by thermal denaturation study using duplex form of calf thymus (CT) DNA.

Keywords: Pyrrolobenzodiazepine, benzimidazoles, cytotoxicity, DNA-binding affinity.

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