5542-60-9Relevant articles and documents
The cisplatin-based Pt(iv)-diclorofibrato multi-action anticancer prodrug exhibits excellent performances also under hypoxic conditions
Gabano, Elisabetta,Ravera, Mauro,Trivero, Francesca,Tinello, Stefano,Gallina, Andrea,Zanellato, Ilaria,Gariboldi, Marzia B.,Monti, Elena,Osella, Domenico
, p. 8268 - 8282 (2018)
Multi-action cisplatin-based mono- (1) and di-clofibric acid (2) Pt(iv) "combo" derivatives were synthesized via both traditional and microwave assisted procedures. The two complexes offered very good performances (IC50 values in a nanomolar ra
Discovery of AdipoRon analogues as novel AMPK activators without inhibiting mitochondrial complex I
Chen, Caiping,Cheng, Keguang,Cheng, Yalong,Dai, Liang,Li, Haobin,Qian, Ming,Sun, Geng,Wang, Pengfei,Wen, Xiaoan,Xu, Qing-Long,You, Yanping,Yuan, Haoliang,Zhou, Xinyu
supporting information, (2020/06/08)
Activation of AMPK emerges as a potential therapeutic approach to metabolic diseases. AdipoRon is claimed to be an adiponectin receptor agonist that activates AMPK through adiponectin receptor 1 (AdipoR1). However, AdipoRon also exhibits moderate inhibition of mitochondrial complex I, leading to increased risk of lactic acidosis. In order to find novel AdipoRon analogues that activate AMPK without inhibition of complex I, 27 analogues of AdipoRon were designed, synthesized and biologically evaluated. As results, benzyloxy arylamide B10 was identified as a potent AMPK activator without inhibition of complex I. B10 dose-dependently improved glucose tolerance in normal mice, and significantly lowered fasting blood glucose level and ameliorated insulin resistance in db/db diabetic mice. More importantly, unlike the pan-AMPK activator MK-8722, B10 did not cause cardiac hypertrophy, probably owing to its selective activation of AMPK in the muscle tissue but not in the heart tissue. Together, B10 represents a novel class of AMPK activators with promising therapeutic potential against metabolic disease.
Acetophenone compounds, preparation methods thereof and application thereof in regulating blood lipid
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Paragraph 0074; 0075; 0076, (2018/09/08)
The invention discloses a compound as shown in formula I or pharmaceutically acceptable salt and a preparation method thereof as well as application thereof in the preparation of drugs for regulatingblood lipid.