44915-39-1Relevant academic research and scientific papers
Design and synthesis of 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles and pyrazolo[3,4-b]pyridines for Aurora-A kinase inhibitors
Shi, Jianyou,Xu, Guobin,Zhu, Wei,Ye, Haoyu,Yang, Shengyong,Luo, Youfu,Han, Jing,Yang, Jincheng,Li, Rui,Wei, Yuquan,Chen, Lijuan
supporting information; experimental part, p. 4273 - 4278 (2010/09/04)
Two series of 3-aminopyrazole compounds including 24 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles and 16 pyrazolo[3,4-b]pyridines were synthesized and evaluated against HCT116, A549, and A2780 tumor cell lines. Among them, three compounds were found to have the ideal anti-proliferative activities in vitro. Docking experiments showed that the novel pyrazolo[3,4-b]pyridines share the similar interaction mode with Aurora-A kinase as PHA739358.
(3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one, a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes
Biftu, Tesfaye,Feng, Dennis,Qian, Xiaoxia,Liang, Gui-Bai,Kieczykowski, Gerard,Eiermann, George,He, Huaibing,Leiting, Barbara,Lyons, Kathy,Petrov, Aleksandr,Sinha-Roy, Ranabir,Zhang, Bei,Scapin, Giovanna,Patel, Sangita,Gao, Ying-Duo,Singh, Suresh,Wu, Joseph,Zhang, Xiaoping,Thornberry, Nancy A.,Weber, Ann E.
, p. 49 - 52 (2007/10/03)
Replacement of the triazolopiperazine ring of sitagliptin (DPP-4 IC50 = 18 nM) with 3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one gave dipeptidyl peptidase IV (DPP-4) inhibitor 1 which is potent (DPP-4 IC50 = 2.6 nM), selective, and ef
Potent and selective aurora inhibitors identified by the expansion of a novel scaffold for protein kinase inhibition
Fancelli, Daniele,Berta, Daniela,Bindi, Simona,Cameron, Alexander,Cappella, Paolo,Carpinelli, Patrizia,Catana, Cornel,Forte, Barbara,Giordano, Patrizia,Giorgini, Maria Laura,Mantegani, Sergio,Marsiglio, Aurelio,Meroni, Maurizio,Moll, Juergen,Pittalà, Valeria,Roletto, Fulvia,Severino, Dino,Soncini, Chiara,Storici, Paola,Tonani, Roberto,Varasi, Mario,Vulpetti, Anna,Vianello, Paola
, p. 3080 - 3084 (2007/10/03)
Potent and selective Aurora kinase inhibitors were identified from the combinatorial expansion of the 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole bi-cycle, a novel and versatile scaffold designed to target the ATP pocket of protein kinases. The most potent c
SYNTHESIS OF N-2-CARBOXYETHYL-N-PHOSPHONOMETHYLGLYCINE
Negrebetskii, Vad. V.,Kolesova, V. A.,Bobkova, R. G.,Chimishkyan, A. L.,Shvetsov-Shilovskii, N. I.
, p. 104 - 108 (2007/10/02)
A method was developed for the synthesis of N-2-carboxyethyl-N-phosphonomethylglycine by phosphonomethylation of N-cyanoethylglycine by the Kabachnik-Fields method, followed by hydrolysis.The reaction of cyanoethylglycine with dimethyl phosphite and a 35percent aqueous solution of formaldehyde was studied by 31P NMR spectroscopy, and the structures of the main and side-reaction products were established.It was shown that the reaction kinetics is described by a second-order reaction.
