Debarshi Kar Mahapatra, Ruchi S Shivhare


Introduction: In the normal course, the activity of murrayanine is very minimal and the most attractive way to improve the anti-proliferative activity involves semi-synthesis. Previously, hybrids of murrayanine (tert-butyl containing, thiazole-linked, uracil-fused) have been screened by our research group which showed promising enhancement (several-folds) in the activity. Objective: In the present research, (E)-1-(1-methoxy-9H-carbazol-3-yl)-3-(4-(methylsulfonyl)phenyl)prop-2-en-1-one was screened against breast cancer cell line MCF-7 employing the SRB assay and studied to establish its IC50 value in comparison with the standard drug. The synergistic anti-cancer activity of the combination of carbazole scaffold (eminent anti-neoplatic effect), murrayanine moiety (fair anti-proliferative agent), chalcone scaffold (prominent anti-cancer activity), and methylsulfonyl component in the para position of the ring-B (high anti-tumor potential) was explored considerably. Results: The anti-breast cancer potential of the substituted murrayanine-chalcone was found to be quite incredible as indicated by the IC50 value of 37.16 μM in comparison with the positive control capecitabine (IC50 value of 6.49 μM). Conclusion: The methylsulfonyl group substituted murrayanine-chalcone scaffold produced noteworthy anti-proliferative activity against breast cancer cell line MCF-7. The present interesting study will inspire the researchers and will positively provide directions towards the future rational development of potential low-molecular-weight ligands with profound anti-cancer activity.

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