Novel benzopsoralen analogues: Synthesis, biological activity and molecular docking studies

Abstract

New benzopsoralen analogues were synthesized and their inhibitory effect on the growth of tumourtumour cell lines (MDA MB231 and TCC-SUP) was evaluated. The in vitro antitumour activity of the new benzopsoralen analogues was discussed in terms of structure-activity relationship. Molecular docking studies with human-CYP2A6 enzymes were also carried out with the synthesized compounds to evaluate the potential of these molecules to interact with the haem group of the enzymes. The results demonstrated that the compounds that are able to interact with the iron ion of the haem cofactor and at the same time with active site Asn297 are those that have better anti-proliferative activity.

Carbazole scaffolds in cancer therapy: a review from 2012 to 2018

“…Every benzosporalen and carbazole derivative showed interesting anti-proliferative activities, with GI 50 values in the nanomolar range against both cell lines. Among carbazole derivatives, compound 6 (Figure 10) had very strong activity with GI 50 values of 0.198 and 0.025 mM against MDA MB231 and TCC-SUP cell lines, respectively 37 .…”

Annulated Heterocyclic[g]Coumarin Composites: Synthetic Approaches and Bioactive Profiling

“…Secondly, the connection between the triazole and dihydropyr-anocoumarin was established via an ether bond at the coumarin nucleus's position C8, rather than a CÀ C bond at C3. A group of compounds (128)(129)(130)(131)(132)(133) among the produced compounds, as shown in Figure 8, showed a moderate degree of growth inhibition against the tested bacterial strains. This was observed by the determination of MIC values, which ranged from 0.075 to 0.17 mg/ml, as well as the measurement of inhibition zones, which fell within the range of 10 to 16 mm.…”