JOURNAL OF CLINICAL AND BIOMEDICAL SCIENCES

Article

Journal of Clinical and Biomedical Sciences

Year: 2025, Volume: 15, Issue: 3, Pages: 184-190

Original Article

Design, Synthesis and Biological Evaluation of Some Novel Benzthiazole Containing 4H-Chromene-4-one Derivatives

Received Date:22 January 2025, Accepted Date:06 March 2025, Published Date:26 September 2025

Abstract

Background: Chromene derivatives are gaining attention in the pharmaceutical industry, while substituted benzothiazole derivatives have shown potential in various therapeutic areas, including anti-ulcer, anti-hypertensive, anti-viral, anti-fungal, anti-cancer, and anti-histaminic treatments. Material and Methods: Benzimidazole derivatives, when combined with other heterocyclic compounds such as pyrazole, thiadiazole, triazole, thiazole, coumarin, and 2-azetidinone, exhibit a wide range of pharmacological properties. In our research, we developed novel 2-(2-(5-nitro-1H-benzo[d]thiazol-2-yl)vinyl)-4H-chromen-4-one derivatives through a reaction involving 2-methyl-1H-benzo[d]thiazole and substituted chromone-3-carbaldehyde in the presence of glacial acetic acid (GAA). Results: The synthesized compounds were characterized using techniques such as IR spectroscopy, ¹H NMR, ¹³C NMR, mass spectrometry, and elemental analysis. Their in-vitro anti-cancer activity was assessed against the A-549 human cancer cell line using the SRB assay method. Among the tested compounds, R1 and R6 demonstrated significant inhibitory activity, reducing cell growth by 21.9% and 39.4%, respectively, at a concentration of 80 µg/mL, while other derivatives allowed 57–94% cell growth. Conclusion: The biological activity was influenced by the substitutions on the coumarin nucleus, with unsubstituted (R4), fluoro-substituted (R6), and chloro-substituted (R1) coumarin derivatives showing notable potency.

Keywords: Synthesis, Heterocyclic, Benzthiazole, Chromene, Derivatives, Cancer cell line

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Copyright

This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.

Published By Sri Devaraj Urs Academy of Higher Education, Kolar, Karnataka

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