Synthesis of novel building blocks of benzosuberone bearing coumarin moieties and their evaluation as potential anticancer agents

• All novel benzosuberone bearing comarin moieties were synthesized.
• Their in vitro cytotoxicity against human A549, HeLa, MDA-MB-231, MCF-7 and normal HEK293 cell line was tested.
• All the synthesised compounds showed cytotoxicity against human cancer and inactive for normal cell line.
• Compound 5a and 5c exhibited significant cytotoxicity against Human breast, alveolar and cervical cell lines.

A series of novel benzosuberone bearing coumarin moieties 5a–c have been synthesized and their structures were determined by analytical and spectral (FT-IR, 1H NMR, 13C NMR, HRMS) studies. The newly synthesized compounds were evaluated for their cytotoxicity against four human cancer cell lines, A549 (Human alveolar adenocarcinoma cell line), HeLa (Human cervical cancer cell line), MDA-MB-231 (Human breast adenocarcinoma cell line), MCF-7 (Human breast adenocarcinoma cell line) and normal cell line HEK293 (Human embryonic kidney cell line). Compound 5a exhibited promising cytotoxicity with IC50 values ranging from 3.35 to 16.79 μM against all the cancer cell lines like A549, HeLa, MCF-7 and MDA-MB-231, while compound 5c showed significant cytotoxicity against HeLa and MDA-MB-231 with IC50 values of 6.72 and 4.87, respectively.

A novel building blocks of benzosuberone bearing coumarin moiety analogues (5a–c) were synthesized and evaluated their cytotoxicity against the human cancer A549, He La, MDA-MB-231, MCF-7 and non cancer HEK293 cell line.Figure optionsDownload as PowerPoint slide