75039-59-7Relevant articles and documents
A one-pot pseudo nine-component isocyanide-based reaction: Synthesis of a new class of zinc 1,5-disubstituted 1H-tetrazol-5-yl coordination complexes
Shaabani, Ahmad,Mahyari, Mojtaba,Seyyedhamzeh, Mozhdeh,Keshipour, Sajjad,Ng, Seik Weng
, p. 4388 - 4391 (2011)
A novel one-pot pseudo nine-component synthesis of zinc 1,5-disubstituted 1H-tetrazol-5-yl coordination complexes in good yields starting from simple and readily available substrates, including a 1,3-dicarbonyl compound, an isocyanide, N,N-dimethylformami
Inhibition studies on carbonic anhydrase isoforms I, II, IV and IX with N-arylsubstituted secondary sulfonamides featuring a bicyclic tetrahydroindazole scaffold
Salerno, Silvia,Amendola, Giorgio,Angeli, Andrea,Baglini, Emma,Barresi, Elisabetta,Marini, Anna Maria,Ravichandran, Rahul,Viviano, Monica,Castellano, Sabrina,Novellino, Ettore,Da Settimo, Federico,Supuran, Claudiu T.,Cosconati, Sandro,Taliani, Sabrina
, (2021)
Carbonic Anhydrases (CAs) are pharmaceutically relevant targets for the treatment of several disease conditions. The ubiquitous localization of these enzymes and the high homology shared by the different isoforms represent substantial impediments for the
Discovery and Optimization of 2 H-1λ2-Pyridin-2-one Inhibitors of Mutant Isocitrate Dehydrogenase 1 for the Treatment of Cancer
Rohde, Jason M.,Karavadhi, Surendra,Pragani, Rajan,Liu, Li,Fang, Yuhong,Zhang, Weihe,McIver, Andrew,Zheng, Hongchao,Liu, Qingyang,Davis, Mindy I.,Urban, Daniel J.,Lee, Tobie D.,Cheff, Dorian M.,Hollingshead, Melinda,Henderson, Mark J.,Martinez, Natalia J.,Brimacombe, Kyle R.,Yasgar, Adam,Zhao, Wei,Klumpp-Thomas, Carleen,Michael, Sam,Covey, Joseph,Moore, William J.,Stott, Gordon M.,Li, Zhuyin,Simeonov, Anton,Jadhav, Ajit,Frye, Stephen,Hall, Matthew D.,Shen, Min,Wang, Xiaodong,Patnaik, Samarjit,Boxer, Matthew B.
, p. 4913 - 4946 (2021/05/07)
Neomorphic mutations in isocitrate dehydrogenase 1 (IDH1) are oncogenic for a number of malignancies, primarily low-grade gliomas and acute myeloid leukemia. We report a medicinal chemistry campaign around a 7,7-dimethyl-7,8-dihydro-2H-1λ2-quinoline-2,5(6H)-dione screening hit against the R132H and R132C mutant forms of isocitrate dehydrogenase (IDH1). Systematic SAR efforts produced a series of potent pyrid-2-one mIDH1 inhibitors, including the atropisomer (+)-119 (NCATS-SM5637, NSC 791985). In an engineered mIDH1-U87-xenograft mouse model, after a single oral dose of 30 mg/kg, 16 h post dose, between 16 and 48 h, (+)-119 showed higher tumoral concentrations that corresponded to lower 2-HG concentrations, when compared with the approved drug AG-120 (ivosidenib).