An article Structure-based design, synthesis, and evaluation of Bcl-2/Mcl-1 dual inhibitors WOS:000530108500008 published article about APOPTOSIS PATHWAYS; BCL-2 FAMILY; CELL-DEATH; CANCER; MCL-1; BCL-X(L); PROTEINS; BIOLOGY in [Zhu, Junjie; Zhang, Xiaodong; Song, Ting; Ji, Tong; Zhang, Zhichao] Dalian Univ Technol, Sch Chem, State Key Lab Fine Chem, Dalian 116012, Peoples R China; [Wang, Ziqian] Dalian Univ Technol, Zhang Dayu Sch Chem, Dalian, Peoples R China; [Guo, Zongwei; Guo, Yafei] Dalian Univ Technol, Sch Life Sci & Technol, Dalian, Peoples R China in 2020.0, Cited 32.0. The Name is Benzyl Alcohol. Through research, I have a further understanding and discovery of 100-51-6. Safety of Benzyl Alcohol
Based on our previously reported Bcl-2/Mcl-1 dual inhibitor 4-thiomorpholinyl-2-cyano-3-amidinophenalenone (A1) that simultaneously occupies the p2 and p4 hydrophobic pockets of Bcl-2 and Mcl-1, we optimized molecules with different bond angles of the groups extending to the p4 pocket and bulky hydrophobic groups to explore p2. Research on structure-activity relationship resulted in a new derivative B4 that is capable of occupying both the p2 and p4 more deeply and completely than A1, with K-i values determined by fluorescence polarization assay (FPAs) improving to 0.31 mu M for Bcl-2 and 0.16 mu M for Mcl-1. Furthermore, B4 exhibited selective lethality on cancer cells over normal cells. It showed stronger apoptosis induction than (-)-gossypol on a Bcl-2/Mcl-1-dependent cancer cell line and killed an Mcl-1-dependent cell line which is resistant to ABT-199 treatment.
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,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles