175152-72-4Relevant academic research and scientific papers
Design, Synthesis, and Evaluation of Reversible and Irreversible Monoacylglycerol Lipase Positron Emission Tomography (PET) Tracers Using a "tail Switching" Strategy on a Piperazinyl Azetidine Skeleton
Chen, Zhen,Mori, Wakana,Deng, Xiaoyun,Cheng, Ran,Ogasawara, Daisuke,Zhang, Genwei,Schafroth, Michael A.,Dahl, Kenneth,Fu, Hualong,Hatori, Akiko,Shao, Tuo,Zhang, Yiding,Yamasaki, Tomoteru,Zhang, Xiaofei,Rong, Jian,Yu, Qingzhen,Hu, Kuan,Fujinaga, Masayuki,Xie, Lin,Kumata, Katsushi,Gou, Yuancheng,Chen, Jingjin,Gu, Shuyin,Bao, Liang,Wang, Lu,Collier, Thomas Lee,Vasdev, Neil,Shao, Yihan,Ma, Jun-An,Cravatt, Benjamin F.,Fowler, Christopher,Josephson, Lee,Zhang, Ming-Rong,Liang, Steven H.
, p. 3336 - 3353 (2019/03/29)
Monoacylglycerol lipase (MAGL) is a serine hydrolase that degrades 2-arachidonoylglycerol (2-AG) in the endocannabinoid system (eCB). Selective inhibition of MAGL has emerged as a potential therapeutic approach for the treatment of diverse pathological co
Discovery of 4-(benzylaminomethylene)isoquinoline-1,3-(2H,4H)-diones and 4-[(pyridylmethyl)aminomethylene]isoquinoline-1,3-(2H,4H)-diones as potent and selective inhibitors of the cyclin-dependent kinase 4
Tsou,Liu, Xiaoxiang,Birnberg, Gary,Kaplan, Joshua,Otteng, Mercy,Tran, Tritin,Kutterer, Kristina,Tang, Zhilian,Suayan, Ron,Zask, Arie,Ravi, Malini,Bretz, Angela,Grillo, Mary,Mcginnis, John P.,Rabindran, Sridhar K.,Ayral-Kaloustian, Semiramis,Mansour, Tarek S.
scheme or table, p. 2289 - 2310 (2010/02/28)
The series of 4-(benzylaminomethylene)isoquinoline-1,3-(2H,4H)-dione and 4-[(pyridylmethyl)aminometh-ylene]isoquinoline-1,3-(2H,4H)-dione derivatives reported here represents a novel class of potential antitumor agents, which potently and selectively inhibit CDK4 over CDK2 and CDK1. In the benzylamino headpiece, a 3-OH substituent is required on the phenyl ring for CDK4 inhibitory activity, which is further enhanced when an iodo, aryl, heteroaryl, t-butyl, or cyclopentyl substituent is introduced at the C-6 position of the isoquinoline-1,3-dione core. To circumvent the metabolic liability associated with the phenolic OH group on the 4-substituted 3-OH phenyl headpiece, we take two approaches: first, introduce a nitrogen o- or p- to the 3-OH group in the phenyl ring; second, replace the phenyl headpiece with N-substituted 2-pyridones. We present here the synthesis, SAR data, metabolic stability data, and a CDK4 mimic model that explains the binding, potency, and selectivity of our CDK4 selective inhibitors.
Benzoheterocyclic derivatives
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Page column 92, (2010/01/21)
A benzoheterocyclic derivative of the following formula [1]: and pharmaceutically acceptable salts thereof, which show excellent anti-vasopressin activity, vasopressin agonistic activity and oxytocin antagonistic activity, and are useful as a vasopressin antagonist, vasopressin agonist or oxytocin antagonist.
