Synthesis, Anticancer Evaluation and SAR-Study of Novel Sulfapyridine Derivatives

Document Type : Original Article

Authors

Chemistry Department, Faculty of Science, Mansoura University

Abstract

This study focuses on developing and evaluating a novel series of sulfapyridine derivatives for their potential as anticancer agents. The strategic starting material, 2-chloro-N-(4-(N-(pyridine-2-yl)sulfamoyl)phenyl)acetamide, served as the foundation for the synthesis of various compounds. Clarifying the synthetic compounds' structures was accomplished through the analysis of IR, 1H NMR, 13C NMR, and MS spectral data.
In vitro screening assays were conducted to assess the freshly generated compounds' anticancer activity in opposition to a panel of human cancer cell lines, which included (HePG-2), (PC-3), (HCT-116), and breast cancer cell lines from the mammary gland (MCF-7). Interestingly, compounds with a thiophene moiety compounds 4 and 8 in particular showed notable activity. Compound 8 demonstrated encouraging results against each of the four cancer cell lines, suggesting its potential as a lead candidate for further expansion as an anti-tumor agent.
This study contributes to understanding the structure-activity relationship of sulfapyridine derivatives and highlights the potential of compound 8 as a valuable applicant for future anticancer drug development.

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