MUMBAI, India, July 7 -- Intellectual Property India has published a patent application (202641060648 A) filed by Christ University on May 13, 2026, for Design,synthesis And In-Vitro Evaluation Of Novel Benzothiazole Coumarin Scaffolds As Potent Cytotoxic Agents Against Hepg2 Cancer Cell Lines.
Inventors include Amruta Kush Durgi; and Ajesh Vijayan.
The application for the patent was published on July 03, 2026, under issue no. 27/2026.
Abstract: Cancer is a life-threatening disease marked by uncontrolled cellular proliferation and invasion of surrounding tissues, leading to a significantly high mortality rate. Hence development of new bioactive compounds is essential in developing anticancer agents targeting multiple pathways involved in cancer. While the development of novel bioactive molecules is crucial, it is equally important that their synthetic routes remain environmentally benign. In the current investigation, we have presented a simple, cost-effective synthesis of new benzothiazole-coumarin hybrids and cytotoxicity evaluation of these molecules against HepG2 cancer cell lines. The invention presents a series of novel 2-amino-4-(benzo[d]thiazoI-2-yl)-5-oxo-4H,5H-pyrano[3,2-c] chromene-3- carbonitrile derivatives (BCl, BC2, BC3, BC6, BC7, BC8). The synthesis ofthe novel compound 2-amino-4-(benzo[d]thiazol-2-yl)-5-oxo-4H,5H- pyrano[3,2-c] chromene-3-carbonitrile, was accomplished via a facile multicomponent reaction involving benzothiazole-2- carbaldehyde, an active methylene compound, and 4-hydroxycoumarin. The reaction proceeded efficiently at room temperature within 10 minutes in acetonitrile, using piperidine as a basic catalyst. The synthesized compounds were evaluated for their anticancer activity against the HepG2 hepatocellular carcinoma cell line. Cytotoxicity assessment was performed using the MTT assay to determine the antiproliferative effects of BCl, BC2, BC3, BC6, BC7, and BC8 following 24 h of exposure to HepG2 cells. Among the series, BCl demonstrated the most pronounced anticancer activity, yielding the lowest ICso value (20.81 pg/mL) and a significant reduction in cell viability at moderate concentrations, thereby highlighting its potential for ftirther anticancer investigation. Compounds BC6 (ICso = 24.08 pg/mL) and BC3 (ICso = 30.91 pg/mL) showed moderate cytotoxic effects, whereas BC2 (ICso = 41.82 pg/mL) required comparatively higher concentrations to elicit similar responses. In contrast, BC7 (ICso ~ 68.51 pg/mL) and BC8 (ICso = 67.81 pg/mL) displayed relatively weak cytotoxic activity, as reflected by their higher ICso values. Keywords: Benzothiazole, Coumarin, Anti- cancer, cytotoxicity
Disclaimer: Curated by HT Syndication.