144825-18-3Relevant academic research and scientific papers
Discovery of potent N-(isoxazol-5-yl)amides as HSP90 inhibitors
Chen, Danqi,Shen, Aijun,Li, Jian,Shi, Feng,Chen, Wuyan,Ren, Jing,Liu, Hongchun,Xu, Yechun,Wang, Xin,Yang, Xinying,Sun, Yiming,Yang, Min,He, Jianhua,Wang, Yueqin,Zhang, Liping,Huang, Min,Geng, Meiyu,Xiong, Bing,Shen, Jingkang
, p. 765 - 781 (2014)
HSP90 is ubiquitously overexpressed in a broad spectrum of human cancers and has been recognized as an attractive target for cancer treatment. Here, we described the fragment screening, synthesis and structure-activity relationship studies of small molecule inhibitors with 4,5-diarylisoxazole scaffold targeting HSP90. Among them, the compound N-(3-(2,4-dihydroxy-5-isopropylphenyl)-4-(4-((4-morpholinopiperidin-1-yl)methyl)phenyl)isoxazol-5-yl)cyclopropanecarboxamide (108) showed high affinity for binding to HSP90 (FP binding assay, IC50 Combining double low line 0.030 μM) and inhibited the proliferation of various human cancer cell lines with averaging GI50 about 88 nM. Compound 108 exhibited its functional inhibition of HSP90 by depleting key signaling pathways and concomitantly elevating of HSP70 and HSP27 in U-87MG cells. Further in vivo studies showed that compound 108 strongly suppressed the tumor growth of human glioblastoma xenograft model U-87MG with T/C Combining double low line 18.35% at 50 mg/kg q3w/2.5w. Moreover, compound 108 also exhibited good pharmacokinetic properties. Together, our study implicates that compound 108 is a promising candidate of HSP90 inhibitor and is currently advanced to preclinical study.
Selective Liquid Phase Hydrogenation of Benzaldehyde to Benzyl Alcohol Over Alumina Supported Gold
Hao, Yufen,Pischetola, Chiara,Cárdenas-Lizana, Fernando,Keane, Mark A.
, p. 881 - 887 (2019/11/03)
Abstract: We report for the first time 100% benzyl alcohol yield from the liquid phase (T = 353?K, P = 9?bar) hydrogenation of benzaldehyde over Au/Al2O3. Under the same reaction conditions, a benchmark Pt/Al2O3
BENZYL-, (PYRIDIN-3-YL)METHYL- OR (PYRIDIN-4-YL)METHYL-SUBSTITUTED OXADIAZOLOPYRIDINE DERIVATIVES AS GHRELIN O-ACYL TRANSFERASE (GOAT) INHIBITORS
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Page/Page column 68; 74, (2019/08/26)
The present invention relates to compounds of general formula (I), wherein the groups R1 and R2 are defined as in claim 1, which have valuable pharmacological properties, in particular bind to ghrelin O-acyl transferase (GOAT) and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular obesity.
Phenyl 1, 2 - isoxazole or phenyl 1, 2 - pyrazole compound and use thereof (by machine translation)
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, (2017/01/19)
The invention discloses the following formula of phenyl 1, 2 - different oxazole or 1, 2 - pyrazole compounds with use. Through the biological activity tests show that, the compound inhibiting heat shock protein 90 activity. Therefore, the invention phenyl 1, 2 - different oxazole or 1, 2 - pyrazole compounds can be used as a heat shock protein 90 inhibitor for the treatment of cancer. (by machine translation)
NOVEL AMIDE COMPOUNDS WITH MCH ANTAGONISTIC EFFECT AND MEDICAMENTS COMPRISING SAID COMPOUNDS
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Page/Page column 100, (2008/06/13)
The invention relates to amide compounds of general formula (I), in which the groups and residues A, B, b, W, X, Y, Z, R1, R2 and R3 have the meanings given in claim 1. The invention further relates to medicaments comprising at least one of said amides. Said medicaments are suitable for the treatment of metabolic disorders and/or eating disorders, in particular, obesity, bulimia, anorexia, hyperphagia, and diabetes as a result of the MCH receptor antagonism.
New carboxamide compounds having melanin concentrating hormone antagonistic activity, pharmaceutical preparations comprising these compounds and process for their manufacture
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Page/Page column 35, (2010/02/09)
The present invention relates to carboxamide compounds of general formula I wherein the groups and residues A, B, W, X, Y, Z, R1, R2, R3 and k have the meanings given in claim 1. Moreover the invention relates to process for preparing the above mentioned carboxamides as well as pharmaceutical compositions containing at least one carboxamide according to the invention. In view of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.
