Authors:

Sebastian Rosario Torres

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About Paper:

Indole-based chalcones are a class of organic compounds that combine the chalcone structure with an indole moiety. These compounds are significant in medicinal chemistry due to their diverse biological activities, including anti-inflammatory, anti-cancer, anti-microbial, and antioxidant properties. Derivatives of indole-based chalcones can be synthesized through various chemical modifications, which can enhance their biological activities or alter their chemical properties for specific applications. Among the prepared N-arylated indolylsulfoXimines, the compound NR07 showed potent and selective cytotoxicity against 22Rv1, C4-2 and MCF7 cells, respectively. IndolylsulfoXimine derivative NR07 displayed a broad spectrum of activity (?M) against the tested cancer cell lines. These compounds were found to be non-cytotoxic to normal HEK293 cells, indicating their potential selectivity for cancer cells. We analyzed the impact of NR07on various cellular assays to uncover its mechanism of action. Cellular assay shows that NR07 increases the endogenous level of ROS, inducing apoptosis. NR07 also induced mitochondrial dysfunction, further promoting apoptotic pathways. Besides, NR07 also restricts cell invasiveness, indicating that it could serve as an effective anti-metastatic agent. As oxidative stress severe F actin causing tubulin depolymerization, we examined the impact of NR07 on tubulin dynamics. Accordingly, NR07treatment decreased the levels of polymerized tubulin in 22Rv1 and C4-2 cells. Although future studies are needed to determine their exact molecular target(s). The IC 50 values of NR-07 in HEK293 is 1.9549 and in MDAMB-231 is 0.7865, our data shows that N-aryl indolylsulfoXimines could serve as effective anti-cancer agents. Keywords: [no keywords provided]

Source:

Purdue University / 2024

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Co-authors:

Sebastian Rosario Torres