On April 1, 2020, Liu, Lulu; Liu, Renshuai; Yang, Xinying; Hou, Xuben; Fang, Hao published an article.Application of 97-09-6 The title of the article was Design, synthesis and biological evaluation of tyrosine derivatives as Mcl-1 inhibitors. And the article contained the following:
The upregulation of the protein myeloid cell leukemia-1 (Mcl-1) is closely associated with various human cancers, which can result in the evasion of apoptosis and a low survival rate. Therefore, developing Mcl-1 inhibitors has become a promising paradigm for cancer therapy. Herein, we designed and synthesized a novel series of tyrosine derivatives, among which compounds (I) (R1 = 3,5-di-Me-4-Cl-Ph, X = H, R2 = OBut, n = 2; R1 = 3,5-di-Me-4-Cl-Ph, X = H, R2 = Ph, n = 1; R1 = naphthyl, X = Br, R2 = 4-Me-benzyl, n = 1) exhibited very high binding affinity to Mcl-1 with Ki values of 0.18, 0.27 and 0.23μM, resp. Interestingly, compound I (R1 = 3,5-di-Me-4-Cl-Ph, X = H, R2 = Ph, n = 1) showed not only potent activity against Mcl-1 but also considerable selectivity over Bcl-2 and Bcl-xL, which was rationalized by mol. docking and fragment-centric topog. mapping (FCTM). It is worth noting that compounds I (R1 = 3,5-di-Me-4-Cl-Ph, X = H, R2 = OBut, n = 2; R1 = 3,5-di-Me-4-Cl-Ph, X = H, R2 = Ph, n = 1; R1 = naphthyl, X = Br, R2 = 4-Me-benzyl, n = 1) displayed potent antiproliferative activity against several cancer cell lines and could induce apoptosis of KM3 and HepG2 cells in a dose-dependent manner. The experimental process involved the reaction of 3-Nitro-4-chlorobenzenesulfonamide(cas: 97-09-6).Application of 97-09-6
The Article related to peptidomimetic tyrosine synthesis drug design apoptosis, mol docking mcl1 inhibitor peptidomimetic, tyrosine methyl ester bromoalkane condensation benzenesulfonamide amidation coupling, apoptosis, cancer, mcl-1 inhibitors, tyrosine derivatives and other aspects.Application of 97-09-6
Referemce:
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