317319-17-8Relevant articles and documents
Microwave Assisted Synthesis and Antibacterial Activity of New 1,3,4-Thiadiazoles and 1,2,4-Triazoles Derived from 2-{2-[2-(4-Fluorophenyl)-4-methylthiazol-5-yl]-1H-benzo[d]imidazol-1-yl}acetohydrazide
Akolkar, H. N.,Burungale, A. S.,Darekar, N. R.,Karale, B. K.
, p. 1721 - 1726 (2020)
Abstract: A series of novel derivatives of1-(2-{2-[2-(4-fluorophenyl)-4-methylthiazol-5-yl]-1H-benzo[d]imidazol-1-yl}acetyl)-4-phenylthiosemicarbazide,5-({2-[2-(4-fluorophenyl)-4-methylthiazol-5-yl]-1H-benzo[d]imidazol-1-yl}methyl)-4-phenyl-4H-1,2,4-triaz
Discovery of 3,5-dimethylisoxazole derivatives as novel, potent inhibitors for bromodomain and extraterminal domain (BET) family
Fang, Lincheng,Hu, Zhaoxue,Yang, Yifei,Chen, Pan,Zhou, Jinpei,Zhang, Huibin
supporting information, (2021/04/15)
Bromodomain and extra-terminal (BET) is a promising therapeutic target for various hematologic cancers. We used the BRD4 inhibitor compound 13 as a lead compound to develop a variety of compounds, and we introduced diverse groups into the position of the compound 13 orienting toward the ZA channel. A series of compounds (14–23, 38–41, 43, 47–49) bearing triazolopyridazine motif exhibited remarkable BRD4 protein inhibitory activities. Among them, compound 39 inhibited BRD4(BD1) protein with an IC50 of 0.003 μM was superior to lead compound 13. Meanwhile, compound 39 possess activity, IC50 = 2.1 μM, in antiproliferation activity against U266 cancer cells. On the other hand, compound 39 could arrest tumor cells into the G0/G1 phase and induce apoptosis, which was consistent with its results in inhibiting cell proliferation. Biological and biochemical data suggest that BRD4 protein might be a therapeutic target and that compound 39 is an excellent lead compound for further development.
Identification of protein tyrosine phosphatase 1B (PTP1B) inhibitors through De Novo Evoluton, synthesis, biological evaluation and molecular dynamics simulation
Dong, Weili,Du, Shan,Li, Weiya,Ma, Yangchun,Sun, Yingzhan,Wang, Runling,Wu, Jingwei,Zhou, Hui,Zhou, Liang
, (2020/03/25)
Protein tyrosine phosphatase 1B (PTP1B) is a widely expressed 50 kDa enzyme and the first intracellular PTP to be purified from human placental tissue. It has been proved that protein tyrosine phosphatase 1B played a significant role in the negative regul