黑色素瘤
细胞培养
细胞生长
毒性
药理学
癌症研究
细胞
医学
化学
生物
内科学
生物化学
遗传学
作者
Anne‐Dorothee Steinkamp,Laurenz Schmitt,Xiaoyun Chen,Katharina Fietkau,Ruth Heise,Jens Malte Baron,Carsten Bolm
摘要
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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