52803-75-5Relevant articles and documents
Synthesis and biological evaluation of novel N-substituted benzamides as anti-migration agents for treatment of osteosarcoma
Chen, Xiaojing,Wang, Guangbao,Mohammed Alsayed, Ali Mohammed,Du, Zongxuan,Lu liu,Ma, Yue,Liu, Peng,Zhang, Qianwen,Chen, Xianxin,Chen, Wenbin,Ye, Faqing,Zheng, Xiaohui,Liu, Zhiguo
, (2021/02/03)
A novel series of novel N-substituted (indole or indazole) benzamides were synthesized, and their anti-tumor properties were evaluated. The majority of tested compounds possessed moderate cytotoxicity, but inspiringly, we verified that active compound 5d presents an astonishing advantage by inhibiting the adhesion, migration, and invasion of osteosarcoma (OS) cells in vitro. Mechanistically, we confirmed 5d inhibited the migration ability of OS cells via the expression of genes related to adhesion, migration, and invasion. This effects of 5d suggest that it can be used as a potential chemotherapeutic drug to some aggressive and/or metastatic cancers, as well as in combination with other clinical anti-cancer drugs. In turn, this could enhance the therapeutic effect or reduce the risk of cell migration.
Discovery of 5-substituent-N-arylbenzamide derivatives as potent, selective and orally bioavailable LRRK2 inhibitors
Ding, Xiao,Dai, Xuedong,Long, Kai,Peng, Cheng,Andreotti, Daniele,Bamborough, Paul,Eatherton, Andrew J.,Edge, Colin,Jandu, Karamjit S.,Nichols, Paula L.,Philps, Oliver J.,Stasi, Luigi Piero,Wan, Zehong,Xiang, Jia-Ning,Dong, Kelly,Dossang, Pamela,Ho, Ming-Hsun,Li, Yi,Mensah, Lucy,Guan, Xiaoming,Reith, Alastair D.,Ren, Feng
, p. 4034 - 4038 (2017/08/23)
Leucine-rich repeat kinase 2 (LRRK2) has been suggested as a potential therapeutic target for Parkinson's disease. Herein we report the discovery of 5-substituent-N-arylbenzamide derivatives as novel LRRK2 inhibitors. Extensive SAR study led to the discovery of compounds 8e, which demonstrated potent LRRK2 inhibition activity, high selectivity across the kinome, good brain exposure, and high oral bioavailability.
NOVEL EP4 RECEPTOR AGONIST COMPOUNDS
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Page/Page column 23, (2009/12/28)
A compound selected from the group consisting of: (3-chloro-4-{[(5-chloro-2-{[(2- chlorophenyl)methyl]oxy}phenyl)carbonyl]amino}phenyl)acetic acid; {4-[({5-chloro-2-[(phenylmethyl)oxy]phenyl}carbonyl)amino]phenyl}acetic acid; {3-chloro-4-[({5-chloro-2-[(phenylmethyl)oxy]phenyl}carbonyl)amino]phenyl}acetic acid; (3-chloro-4-{[(5-chloro-2-{[(3- chlorophenyl)methyl]oxy}phenyl)carbonyl]amino}phenyl)acetic acid; {4-[({2-[(phenylmethyl)oxy]phenyl}carbonyl)amino]phenyl}acetic acid; (4-{[(5-chloro-2-{[(3-chlorophenyl)methyl]oxy}phenyl)carbonyl]amino}-2- fluorophenyl)acetic acid; {3-chloro-4-[({2-[(phenylmethyl)oxy]phenyl}carbonyl)amino]phenyl}acetic acid; (3-chloro-4-{[(2-{[(3-chlorophenyl)methyl]oxy}phenyl)carbonyl]amino}phenyl)acetic acid; {4-[({2-chloro-6-[(phenylmethyl)oxy]phenyl}carbonyl)amino]phenyl}acetic acid; (4-{[(2-chloro-6-{[(3-chlorophenyl)methyl]oxy}phenyl)carbonyl]amino}phenyl)acetic acid; {4-[({5-chloro-2-[(phenylmethyl)amino]phenyl}carbonyl)amino]phenyl}acetic acid; (4-{[(5-chloro-2-{[(3-chlorophenyl)methyl]amino}phenyl)carbonyl]amino}phenyl)acetic acid; and (4-{[(5-chloro-2-{[(2-chlorophenyl)methyl]amino}phenyl)carbonyl]amino}phenyl)acetic acid, or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising such compounds and the use of such compounds in medicine.