174666-16-1Relevant articles and documents
Novel PHD2/HDACs hybrid inhibitors protect against cisplatin-induced acute kidney injury
Wei, Huiqiang,Gou, Wenfeng,Gao, Jun,Ning, Hongxin,Song, Yang,Li, Deguan,Qin, Yong,Hou, Wenbin,Li, Yiliang
, (2022/01/19)
Acute kidney injury (AKI) is associated with high morbidity and mortality. Cisplatin is a common chemotherapeutic, but its nephrotoxicity-driven AKI limits its clinical application. Currently, there are no specific and satisfactory therapies in the clinic for AKI. Inhibitors of hypoxia-inducible factor prolyl hydroxylase 2 (HIF-PHD2) or histone deacetylase (HDACs) had shown renoprotective effects against AKI in preclinical studies. This study aimed to develop a novel therapeutic to prevent AKI progression by targeting PHD2 and HDACs simultaneously. We designed and synthesized a series of PHD2/HDACs hybrid inhibitors. The initial drug activity screening identified a candidate compound 31c, which exhibited potent inhibitory activities against PHD2 and HDAC1/2/6. Cellular analyses further showed that 31c did not affect cisplatin's antitumor activity in cancer cells but strongly protected cisplatin-induced toxicity on HK-2 cells. In vivo studies with the cisplatin-induced AKI mouse model demonstrated that 31c remarkably alleviated kidney dysfunction with suppressed plasma BUN/SCr and increased EPO levels. The potent renoprotective effects of 31c on AKI were confirmed by significant improvements in pathological kidney conditions in the mouse model. These results suggest that the novel PHD2/HDACs hybrid inhibitor, 31c, has a clinical potential as the renoprotective agent for the treatment/prevention of cisplatin-induced AKI for various cancers.
NOVEL CROSSLINKED ALGINIC ACID
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Paragraph 0217-0220, (2021/04/23)
The present invention provides alginic acid derivatives represented by formula (I) and formula (II), and a novel crosslinked alginic acid obtained by carrying out a Huisgen reaction using an alginic acid derivative of formula (I) and an alginic acid derivative of formula (II). There are thereby provided novel alginic acid derivatives and a novel crosslinked alginic acid.
A method for preparing ilastatin is disclosed. Preparation method of intermediate and intermediate
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Paragraph 0048; 0062-0063, (2021/10/27)
The preparation method comprises the following steps: (1) the first intermediate 3 - (dimethylamino) methyl) benzofuran -2 - carboxylic acid and second intermediate 4 - (2 - aminoethoxy) methyl benzoate are subjected to amide condensation to obtain third
Structure-Based Design of Dual-Acting Compounds Targeting Adenosine A2AReceptor and Histone Deacetylase as Novel Tumor Immunotherapeutic Agents
Yan, Wenzhong,Ling, Lijun,Wu, Yiran,Yang, Kexin,Liu, Ruiquan,Zhang, Jinfeng,Zhao, Simeng,Zhong, Guisheng,Zhao, Suwen,Jiang, Hualiang,Xie, Chengying,Cheng, Jianjun
, p. 16573 - 16597 (2021/12/02)
Adenosine is an immunosuppressive factor in the tumor microenvironment mainly through activation of the A2A adenosine receptor (A2AR), which is a mechanism hijacked by tumors to escape immune surveillance. Small-molecule A2AR antagonists are being evaluat
Dual inhibitor for prolyl hydroxylase and histone deacetylase, preparation method and application thereof
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Paragraph 0084; 0085; 0086; 0099; 0100; 0101, (2019/02/04)
The invention discloses a new dual inhibitor for prolyl hydroxylase and histone deacetylase shown as formula I, a preparation method and an application thereof. The new dual inhibitor is capable of selectively promoting the level of hypoxia-inducible fact
Sustainable poly(ether amide)s from lignin-derived precursors
Saenz, Guery,Scott, Colleen
, p. 2154 - 2160 (2018/10/05)
In recent years, there have been concerted efforts to replace petrochemical products with those from renewable sources due to the unsustainability of petroleum feedstock, and the continued volatility in the price. This work describes the synthesis and thermal properties of two new lignin-derived poly(ether-amide)s as alternative thermoplastics to petroleum-based commodities. Poly-4-(2-aminoethoxy)benzoate (PEAB) and poly-4-(2-aminoethoxy)-3-methoxybenzoate (PEAV) are synthesized by a melt polycondensation and characterized by 1H NMR spectroscopy and thermal analysis. The number average molecular weight (Mn) of the polymers are estimated from the 1H NMR spectroscopy analysis, and were shown to be 4100 and 12,000 g/mol for PEAB and PEAV respectively. The PEAB had a higher decomposition temperature (Td) as well as glass transition temperature (Tg) compared to PEAV; albeit, with a lower molecular weight. The polymers’ Td were in the range of 330 °C–380 °C and the Tg were between 100 °C and 120 °C. The thermal properties of the polymers are in the desirable range for thermoplastic materials used in the packaging, storage, and coating industries. Furthermore, the polymers are susceptible to degradation under acidic conditions in a short period; a property that is highly desirable for degradable polymers.
Novel hydroxamates as therapeutic agents
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Page/Page column 18, (2010/02/14)
The present invention is directed to certain hydroxamate derivatives that are inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes f
Nonpeptide α(v)β3 antagonists. 1. Transformation of a potent, integrin-selective α(IIb)β3 antagonist into a potent α(v)β3 antagonist
Duggan,Duong,Fisher,Hamill,Hoffman,Huff,Ihle,Leu,Nagy,Perkins,Rodan,Wesolowski,Whitman,Zartman,Rodan,Hartman
, p. 3736 - 3745 (2007/10/03)
Modification of the potent fibrinogen receptor (α(IIb)β3) antagonist 1 generated compounds with high affinity for the vitronectin receptor α(v)β3. Sequential modification of the basic N-terminus of 1 led to the identification of the
β-adrenergic agonists
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, (2008/06/13)
β-adrenergic agonists for the treatment of diseases/conditions such as obesity and diabetes. The compounds have formula (I), wherein R1, R2, R3, R4, R5, R6, R7, W, X, Y and Z are as defined in the specification.
