99070-16-3Relevant academic research and scientific papers
Reactivity of substrates with multiple competitive reactive sites toward NBS under neat reaction conditions promoted by visible light
Grjol, Bla?,Jereb, Marjan
, p. 5235 - 5248 (2021/06/07)
Regioselectivity of visible-light-induced transformations of a range of (hetero)aryl alkyl-substituted ketones bearing several competitive reactive sites (α-carbonyl, benzyl and aromatic ring) with N-bromosuccinimide (NBS) was studied under solvent-free reaction conditions (SFRC) and in the absence of inert-gas atmosphere, radical initiators and catalysts. An 8-W energy-saving household lamp was used for irradiation. Heterogeneous reaction conditions were dealt with throughout the study. All substrates were mono- or dibrominated at the α-carbonyl position, and additionally, some benzylic or aromatic bromination was observed in substrates with benzylic carbon atoms or electron-donating methoxy groups, respectively. Surprisingly, ipso-substitution of the acyl group with a bromine atom took place with (4-methoxynaphthyl) alkyl ketones. While the addition of the radical scavenger TEMPO (2,2,6,6-tetramethylpiperidin-1-yloxy) decreased the extent of α- and ring bromination, it completely suppressed the benzylic bromination and α,α-dibromination with NBS under SFRC.
Discovery of 5,6-Bis(4-methoxy-3-methylphenyl)pyridin-2-amine as a WSB1 Degrader to Inhibit Cancer Cell Metastasis
Che, Jinxin,Jin, Zegao,Yan, Fangjie,You, Jieqiong,Xie, Jiangfeng,Chen, Binhui,Cheng, Gang,Zhu, Hong,He, Qiaojun,Hu, Yongzhou,Yang, Bo,Cao, Ji,Dong, Xiaowu
, p. 8621 - 8643 (2021/06/28)
The gain of cell motility is an essential prerequisite for cancer metastasis. The ubiquitin ligase subunit WD repeat and SOCS box-containing 1 (WSB1) has been demonstrated to regulate hypoxia-driven tumor cell migration. However, there is still a lack of methods for discovering inhibitors targeting the WSB1 axis. Here, we employed phenotypic screening models and identified compound4that displayed migration inhibitory activity against WSB1-overexpressing cells. Further studies indicated that it may function as a WSB1 degrader, thus leading to the accumulation of the Rho guanosine diphosphate dissociation inhibitor 2 (RhoGDI2) protein, reversing the expression of downstream F-actin and formation of membrane ruffles, and disturbing the migration capacity of cancer cells. Moreover, compound4exhibited a promisingin vivoanticancer metastatic effects. Our findings show the discovery of a new WSB1 degrader, providing a unique solution for the treatment of cancer metastasis.
Identification of a novel selective small-molecule inhibitor of protein arginine methyltransferase 5 (PRMT5) by virtual screening, resynthesis and biological evaluations
Zhu, Kongkai,Jiang, Chengshi,Tao, Hongrui,Liu, Jingqiu,Zhang, Hua,Luo, Cheng
supporting information, p. 1476 - 1483 (2018/04/20)
As one of the most promising anticancer target in protein arginine methyltransferase (PRMT) family, PRMT5 has been drawing more and more attentions, and many efforts have been devoted to develop its inhibitors. In this study, three PRMT5 inhibitors (9, 16
URAT1 inhibitor and its application
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Paragraph 0168-0169, (2018/08/04)
The invention discloses a URAT1 inhibitor compound and its application of the compound. The URAT1 inhibitor compound is the compound or its pharmaceutically acceptable salt shown in structure of Formula (I). The experiment shows that the compound provided
URAT1 inhibitor for promoting uric acid excretion
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Paragraph 0128; 0129; 0130, (2018/09/21)
The invention belongs to the field of medicinal chemistry, and in particular relates to a URT1 inhibitor for promoting uric acid excretion, which is a compound represented by the structure of the formula (I) or a pharmaceutically acceptable salt thereof. Experiments show that the compound provided by the invention has excellent inhibitory effect to hURAT1 transport uric acid in HEK293 transfectedcells and has a good application prospect in treatment of hyperuricemia or gout. The formula (I) is shown in the description.
IMIDAZOLECARBOXAMIDES AND THEIR USE AS FAAH INHIBITORS
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Page/Page column 14; 15, (2015/02/19)
A compound having a structure selected from the following: or a pharmaceutically acceptable salt thereof. The compound may be used as an inhibitor of fatty acid amide hydrolase.
AMINE COMPOUND AND USE THEREOF FOR MEDICAL PURPOSES
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Page/Page column 64, (2008/12/08)
A novel amine compound represented by the following formula (I), which is superior in immunosuppressive action, rejection suppressive action and the like, and shows reduced side effects such as bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or hydrates thereof, or solvate, as well as a pharmaceutical composition containing this compound and a pharmaceutically acceptable carrier. wherein R is a hydrogen atom or P(=O)(OH)2, X is an oxygen atom or a sulfur atom, Y is CH2CH2 or CH=CH, R1 is cyano or alkyl having a carbon number of 1 to 4 and substituted by a halogen atom(s), R2 is alkyl having a carbon number of 1 to 4 and optionally substituted by a hydroxyl group(s) or a halogen atom(s), R3 and R4 may be the same or different and each is a hydrogen atom or alkyl having a carbon number of 1 to 4, and n is 5 - 8.
