Background: Breast cancer is the most common invasive cancer in female worldwide. Indole
scaffold represents an important class of therapeutic agents in medicinal chemistry. Many indole derivatives
are reported as potent anticancer agents. This study aims to design, and synthesize anti-breast cancer
potential of new bisindole derivatives.
Method: The target molecules were prepared by reacting cyano acetyl indoles with substituted indole-3-
carboxyaldehydes in the presence of piperidine. All the newly synthesized compounds were in vitro
screened for their anticancer activities against breast carcinoma (MCF-7) by employing the sulforhodamine
B (SRB) assay method.
Results: Preliminary in vitro evaluation indicated that most of the compounds possess distinct cytotoxicity
profile against MCF-7 cell line compared to standard drug adriamycin. Among them, compounds
5g, 5b, and 5q demonstrated excellent activities against breast carcinoma (GI50 < 0.1µM) as good as
adriamycin (GI50 < 0.1µM). Active compounds were further subjected for molecular docking and
bioavailability studies. These studies supported activities of the present series compounds.
Conclusion: New anti-breast cancer agents are the need of time, we believe that the new α-cyano substituted
1,3-bisindolyl-2-propen-1-one derivative 5g reported in this work may provide an interesting
insight for further optimization.