Abstract
Numerous carbazole derivatives were designed by the Chemsketch software followed by 3D optimization. Docking studies were performed using AUTODOCK 4.2.6 software to check their binding interactions with eukaryotic topoisomerase-I, based on the crystal structure of Human Topoisomerse-I-DNAcomplex (PDB ID: 1A35). Results of docking studies of designed carbazole derivatives were compared on the basis of their minimum binding energy with a well known topoisomerase-I inhibitor i.e. Rebeccamycin,. Above results were used to find out active compounds and two series of such active compounds i.e. 2-[(4, 5-dihydro-2-substitutedphenyl)imidazol-1-ylamino]-1-(9H-carbazol-9-yl)ethanone (3a-3e) and 2-(9H-carbazol-9-yl)-N'-[{(4-substitutedphenyl)(piperazin-1-yl)}methyl]acetohydrazide (3a-3e) were synthesized. All the synthesized compounds were characterized by IR, 1H NMR, 13C NMR, MASS spectrometry and elemental analysis and also screened for their invitro anticancer activity against human breast cancer cell line (MCF 7) by sulphorodamine B (SRB) assay method. GI50 was measured by using 10, 20, 40 and 80 g/ml concentrations of tested compounds along with the standard i.e. Rebeccamycin. Results revealed that the tested compounds 3c, 3e, and 3a were comparable to Adriamycin having GI50<10g/ml. Compound 3c and 3a were found to be most active among all the tested compounds.
Published Version
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