《Discovery and Characterization of 2,5-Substituted Benzoic Acid Dual Inhibitors of the Anti-apoptotic Mcl-1 and Bfl-1 Proteins》 was published in Journal of Medicinal Chemistry in 2020. These research results belong to Kump, Karson J.; Miao, Lei; Mady, Ahmed S. A.; Ansari, Nurul H.; Shrestha, Uttar K.; Yang, Yuting; Pal, Mohan; Liao, Chenzhong; Perdih, Andrej; Abulwerdi, Fardokht A.; Chinnaswamy, Krishnapriya; Meagher, Jennifer L.; Carlson, Jacob M.; Khanna, May; Stuckey, Jeanne A.; Nikolovska-Coleska, Zaneta. Computed Properties of C4H3ClO2S2 The article mentions the following:
Anti-apoptotic Bcl-2 family proteins are overexpressed in a wide spectrum of cancers and have become well validated therapeutic targets. Cancer cells display survival dependence on individual or subsets of anti-apoptotic proteins that could be effectively targeted by multimodal inhibitors. We designed a 2,5-substituted benzoic acid scaffold that displayed equipotent binding to Mcl-1 and Bfl-1. Structure-based design was guided by several solved cocrystal structures with Mcl-1, leading to the development of compound 24, which binds both Mcl-1 and Bfl-1 with Ki values of 100 nM and shows appreciable selectivity over Bcl-2/Bcl-xL. The selective binding profile of 24 was translated to on-target cellular activity in model lymphoma cell lines. These studies lay a foundation for developing more advanced dual Mcl-1/Bfl-1 inhibitors that have potential to provide greater single agent efficacy and broader coverage to combat resistance in several types of cancer than selective Mcl-1 inhibitors alone. After reading the article, we found that the author used Thiophene-2-sulfonyl chloride(cas: 16629-19-9Computed Properties of C4H3ClO2S2)
Thiophene-2-sulfonyl chloride(cas: 16629-19-9) is a member of sulfonyl chlorides. Sulfonyl chlorides are reactive sulfonic acid derivatives similar in properties and reactivity to acid chlorides of carboxylates. The sulfonic acid group, however, is a highly hindered molecule, containing a tetrahedral configuration of substituents. Computed Properties of C4H3ClO2S2
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics