The present work intends to synthesize a new class of small molecules featuring the quinoxaline scaffold. The indolo [2,3-b]quinoxaline-Mannich adducts were designed, synthesized and their anticancer activities were tested using MTS assay against human ovarian cancer (OVCAR-3) and female colorectal adenocarcinoma cancer cell lines (HT-29). Compounds 6q and 6r efficiently inhibited both cancer cell lines tested, with IC50 values of 58.57 and 55.90 µM against OVCAR-3 and 31.36 and 42.3 µM against HT-29, respectively. The evaluation results were further supported by caspase-mediated apoptosis and docking studies, which indicated that Tyr1159 and the N-atom of the pyrrolidine moiety formed an additional hydrogen bond that stabilised the c-Met-kinase-6q complex. Overall, the results of our study suggested that Mannich-inspired indolo [2,3-b]quinoxaline adduct might make interesting lead for the development of cancer chemotherapeutics.
All Science Journal Classification (ASJC) codes
- Analytical Chemistry
- Organic Chemistry
- Inorganic Chemistry