2849-93-6Relevant articles and documents
Structure-based design of novel benzimidazole derivatives as PIN1 inhibitors
Wang, Shuxiang,Guan, Lihong,Zang, Jie,Xing, Kun,Zhang, Jian,Liu, Dan,Zhao, Linxiang
, (2019)
Peptidyl-prolyl cis/trans isomerase Pin1 plays a key role in amplifying and translating multiple oncogenic signaling pathways during oncogenesis. The blockade of Pin1 provided a unique way of disrupting multiple oncogenic pathways and inducing apoptosis. Aiming to develop potent Pin1 inhibitors, a series of benzimidazole derivatives were designed and synthesized. Among the derivatives, compounds 6h and 13g showed the most potent Pin1 inhibitory activity with IC50 values of 0.64 and 0.37 μM, respectively. In vitro antiproliferative assay demonstrated that compounds 6d, 6g, 6h, 6n, 6o and 7c exhibited moderate antiproliferative activity against human prostate cancer PC-3 cells. Taken together, these unique benzimidazole derivatives exhibited great potential to be further explored as potent Pin1 inhibitors with improved potency.
Green synthesis of 1,1-Carbonyldiimidazole using copper oxide nanofiber as a heterogeneous catalyst
Sukumar, Thenmozhi,Nallasamy, Dharmaraj
, p. 234 - 241 (2018)
Poly(vinyl pyrrolidone) (PVP)/copper oxide composite nanofibers were prepared by electrospinning technique using PVP and copper acetate as precursors and calcinated at high temperature to yield polymer free, phase pure copper oxide nanofibers (CuO NFs). T
Discovery of heterocyclic carbohydrazide derivatives as novel selective fatty acid amide hydrolase inhibitors: design, synthesis and anti-neuroinflammatory evaluation
Hao, Qingjing,He, Mengting,Jiang, Kaixuan,Shang, Yanguo,Wang, Jinxin
supporting information, (2020/04/08)
Fatty acid amide hydrolase (FAAH) is a promising target for the development of drugs to treat pain, inflammation, and other central nervous system disorders. Herein, a series of novel heterocyclic carbohydrazide derivatives were firstly designed by the classic scaffold-hopping strategy. Then, multi-steps synthesis and human FAAH enzyme inhibiting activity assays were conducted. Among them, compound 26 showed strong inhibition against human FAAH with IC50 of 2.8 μM. Corresponding docking studies revealed that the acyl hydrazide group of compound 26 well-occupied the acyl-chain binding pocket. It also exhibited high selectivity towards FAAH when comparing with CES2 and MAGL. Additionally, compound 26 effectively suppressed the LPS-induced neuroinflammation of microglial cells (BV2) via the reduction of interleukin-1β and tumor necrosis factor-α. Our results provided significative lead compounds for the further discovery of novel selective and safe FAAH inhibitors with potent anti-neuroinflammation activity.
Substituted heterocyclic compound containing acylhydrazone skeleton as well as preparation method and application thereof (by machine translation)
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Paragraph 0056-0057; 0061-0063, (2019/09/14)
The invention discloses a substituted heterocyclic compound containing an acylhydrazone skeleton as well as a preparation method and application, of the substituted heterocyclic compound. The invention relates to the field, in particular to a substituted heterocyclic compound containing an acylhydrazone skeleton or a pharmaceutically acceptable salt, a pharmaceutical composition containing the compounds and medical application, in particular to an FAAH inhibitor, and application, in preparation of drugs for preventing or treating diseases related to FAAH, including depression, analgesia, cannabinoid use disorders and other related diseases. (by machine translation)
