title: Synthesis of a Sulfonimidamide-Based Analog of Tasisulam and Its Biological Evaluation in the Melanoma Cell Lines SKMel23 and A375.
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.
authors.affiliation: Institute of Organic Chemistry, RWTH Aachen University, Aachen, Germany.
authors.forename: Anne-Dorothee
authors.initials: AD
authors.lastname: Steinkamp
authors.forename: Laurenz
authors.initials: L
authors.lastname: Schmitt
authors.forename: Xiaoyun
authors.initials: X
authors.lastname: Chen
authors.forename: Katharina
authors.initials: K
authors.lastname: Fietkau
authors.forename: Ruth
authors.initials: R
authors.lastname: Heise
authors.forename: Jens M
authors.initials: JM
authors.lastname: Baron
authors.forename: Carsten
authors.initials: C
authors.lastname: Bolm
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001549:Benzamides / Q000138:chemical synthesis* / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D006801:Humans; D008545:Melanoma; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology*
chemical_list: D000970:Antineoplastic Agents; D001549:Benzamides; D013449:Sulfonamides