Sulfonylguanidine Derivatives as Potential Antimelanoma Agents.,ChemMedChem

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Sulfonylguanidine Derivatives as Potential Antimelanoma Agents.
ChemMedChem ( IF 3.6 ) Pub Date : 2020-04-29 , DOI: 10.1002/cmdc.202000218
Tom Baladi ₁ , Nedra Hamouda-Tekaya ₂ , Leticia Christina Pires Gonçalves ₁ , Stéphane Rocchi ₂ , Cyril Ronco ₁ , Rachid Benhida _{1,

3}

Affiliation

Sulfonylguanidines are interesting bioactive compounds with a broad range of applications in the treatment of different pathologies. 2‐Aminobenzazole‐based structures are well employed in the development of new anticancer drugs. Two series of novel N‐benzazol‐2‐yl‐N′‐sulfonyl guanidine derivatives were synthesized with the sulfonylguanidine in either an extra‐ or intracyclic frame. They were evaluated for their antiproliferative activity against malignant melanoma tumor cells, thus allowing structure‐activity relationships to be defined. Additionally, NCI‐60 screening was performed for the best analogue to study its efficiency against a panel of other cancer cell lines. The stability profile of this promising compound was then validated. During the synthetic process, an unexpected new deamidination of the sulfonylguanidine towards sulfonamide function was also identified.

中文翻译：

磺酰胍衍生物作为潜在的anlanlanoma剂。

磺酰胍是令人感兴趣的生物活性化合物，在治疗不同病理方面具有广泛的应用。基于2-氨基苯并唑的结构在开发新的抗癌药物中得到了很好的利用。两个新的N-苯并唑-2-基-N'系列磺酰基胍衍生物是在环外或环内构架与磺酰基胍合成的。评估了它们对恶性黑色素瘤肿瘤细胞的抗增殖活性，从而确定了结构-活性关系。此外，对最佳类似物进行了NCI-60筛选，以研究其对其他癌细胞系的功效。然后验证了该有前途的化合物的稳定性。在合成过程中，还发现了磺酰胍对磺酰胺功能的意外新的脱酰胺基作用。

更新日期：2020-07-03

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