Recommanded Product: 385-00-2. Authors Lin, TT; Li, JC; Liu, LP; Li, YQ; Jiang, HL; Chen, KX; Xu, P; Luo, C; Zhou, B in ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER published article about in [Lin, Tingting; Jiang, Hualiang; Chen, Kaixian; Luo, Cheng] ShanghaiTech Univ, Shanghai Inst Adv Immunochem Studies, Shanghai 200031, Peoples R China; [Lin, Tingting; Jiang, Hualiang; Chen, Kaixian; Luo, Cheng] ShanghaiTech Univ, Sch Life Sci & Technol, Shanghai 200031, Peoples R China; [Lin, Tingting; Li, Jiacheng; Liu, Liping; Li, Yuanqing; Jiang, Hualiang; Chen, Kaixian; Xu, Pan; Luo, Cheng] Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Ctr Chem Biol,Drug Discovery & Design Ctr, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China; [Lin, Tingting; Zhou, Bing] Chinese Acad Sci, Shanghai Inst Mat Med, Dept Med Chem, State Key Lab Drug Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China; [Lin, Tingting; Li, Jiacheng; Liu, Liping; Li, Yuanqing; Jiang, Hualiang; Chen, Kaixian; Luo, Cheng; Zhou, Bing] Univ Chinese Acad Sci, 19 Yuquan Rd, Beijing 100049, Peoples R China in 2021, Cited 39. The Name is 2,6-Difluorobenzoic acid. Through research, I have a further understanding and discovery of 385-00-2
Cyclin-dependent kinases play significant roles in cell cycle progression and are promising targets for cancer therapy. However, most potent CDK inhibitors lack the balance between efficacy and safety because of poor selectivity. Given the roles of CDK2 in tumorigenesis, selective CDK2 inhibition may provide therapeutic benefits against certain cancer. In this study, a series of 4-benzoylamino-1H-pyrazole-3-carboxamide derivatives were designed, synthesized, and evaluated. The most selective compound DC-K2in212 in this series exhibited high potency towards CDK2 and had effective anti-proliferative activity against A2058 melanoma cell line and MV4-11 leukemia cell line while exhibiting low toxic effect on human normal cell lines MRC5 and LX2. The molecular modeling illustrated that compound DC-K2in212 had the similar binding mode with CDK2 as C-73, the most selective CDK2 inhibitor reported so far, which might account for selectivity against CDK2 over CDK1. Further biological studies revealed that compound DC-K2in212 suppressed CDK2-associated downstream signaling pathway, blocked cell cycle progression, and induced cellular apoptosis. Therefore, compound DC-K2in212 could serve as a potential CDK2 inhibitor for further development. (c) 2021 Elsevier Masson SAS. All rights reserved.
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Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com