AI Article Synopsis
- Tasisulam is an antitumor agent used to treat metastatic melanoma and other solid tumors, but its effectiveness is hampered by toxic side effects due to poor clearance in the body.
- Researchers developed a new sulfonimidamide-based analog to improve the drug's effectiveness and reduce toxicity.
- In tests with melanoma cell lines SKMel23 and A375, the new analog showed similar antiproliferative effects to tasisulam, suggesting potential for safer clinical use in future trials.
Article Abstract
Tasisulam is a promising antitumor agent with complex pharmacology, which is used as an antiproliferative agent in patients with metastatic melanoma and other solid tumors. Phase 2 melanoma studies showed promising results but had to be stopped because of insufficient tasisulam clearance leading to toxic side effects. To reduce the negative effects of tasisulam, we synthesized a novel sulfonimidamide-based analog to evaluate its antiproliferative effects in comparison to the original compound by performing a cell proliferation assay in melanoma cell lines SKMel23 and A375. The results revealed that the analog had inhibitory effects on the proliferation comparable to tasisulam in both investigated cell lines. These results could contribute to a reduced toxicity of tasisulam and lead to further clinical trials in metastatic melanoma.
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| http://dx.doi.org/10.1159/000453042 | DOI Listing |
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