Coumarin pharmacophore is a six-membered aromatic heterocyclic, which is present in many natural products and synthetic molecules Coumarins, are widely abundant natural heterocyclic compounds, are extensively employed in creating various biologically potent substances. Coumarin sulfonamide hybrids are excellent compounds which have several applications in pharmacology; such as anti-inflammatory, antioxidant, anti-viral, anti-fungal, anti-bacterial, and anti-cancer properties. The many substitutions around the coumarin sulfonamide nucleus are outlined and by offering a broad range of pharmacological potential, have drawn the interest of numerous researchers that are trying to employ the coumarin sulfonamide hybrids in medication design and the creation of new medicinal compounds. A wide range of medicines, particularly in the fields of oncology and carbonic anhydrase inhibitors, are made possible by advancements in the synthesis and medicinal chemistry of compounds based on coumarin sulfonamide. The production and particular biological actions of several coumarin derivatives are the main topics of this review study. To find and create new synthetic strategies that could aid in structure-activity relationship (SAR) studies, certain innovative research approaches are also mentioned. The anticancer potential of coumarins has drawn attention from researchers recently because of their strong biological activity and low toxicity. Coumarins are frequently used to treat leukemia, prostate cancer, and renal cell carcinoma. They can also be used to reduce the negative effects of radiation therapy. Due to its therapeutic potential in cancer treatment and photo-chemotherapy, coumarin derivatives, both natural and synthetic, are gaining curiosity.

Today Cancer remains to be one of the most deadly diseases in the world. Due to the potential anticancer activity of the chalcone and sulfonamide moieties, five novel hybrid compounds containing both structures have been designed and synthesized in 3 steps. The synthesized compounds were established on the basis of IR, 1H NMR, 13C NMR spectral data, and elemental analysis and also they were screened for in-vitro anticancer activity on human breast cancer cell line MCF-7. Among them, (E) –2–methoxy– N – (4–methoxyphenyl) –5– (3– (4–nitrophenyl) acryloyl) benzene sulfonamide (4) showed the most potent anticancer activity against MCF-7 cell line

We report herein the synthesis of ¾ substituted benzene sulfonamides linked via phenyl ring to a benzothiazole moiety. The title compounds in the two series namely N-(4-(benzothiazole-2-yl) phenyl) 4-substituted benzene sulfonamides and N-(4-(benzothiazole-2-yl) phenyl) 3-substituted benzene sulfonamides were synthesized by condensing 2-(3/4-aminophenyl) benzothiazole with various substituted sulfonyl chlorides. The synthesized compounds were subjected to neurotoxicity screening, computational studies, and evaluation of their anticonvulsant potential. Amongst all the synthesized compounds, compound 9 emerged as the most potent anticonvulsant agent in maximal electroshock (MES) model (standard: phenytoin) in mice and showed three hydrogen bond interactions with the nicotinic acetylcholine ion gated receptors (PDB ID: 2BG9). Interestingly, compound 13 showed five hydrogen bond interactions with the target protein and thus excellent binding affinity upon computational analysis but was found to be neurotoxic.