TY - JOUR
T1 - Synthesis, DNA binding ability and anticancer activity of 2-heteroaryl substituted benzimidazoles linked pyrrolo[2,1-c][1,4]benzodiazepine conjugates
AU - Kamal, Ahmed
AU - Pogula, Praveen Kumar
AU - Khan, Mohammed Naseer Ahmed
AU - Seshadri, Bobburi Naga
AU - Sreekanth, Kokkonda
PY - 2013/8/1
Y1 - 2013/8/1
N2 - 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.
AB - 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.
KW - Benzimidazoles
KW - Cytotoxicity
KW - DNA-binding affinity
KW - Pyrrolobenzodiazepine
UR - http://www.scopus.com/inward/record.url?scp=84883352391&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84883352391&partnerID=8YFLogxK
U2 - 10.2174/1573406411309050004
DO - 10.2174/1573406411309050004
M3 - Article
C2 - 23301523
AN - SCOPUS:84883352391
SN - 1573-4064
VL - 9
SP - 651
EP - 659
JO - Medicinal chemistry
JF - Medicinal chemistry
IS - 5
ER -