- Design and synthesis of 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles and pyrazolo[3,4-b]pyridines for Aurora-A kinase inhibitors
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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.
- Shi, Jianyou,Xu, Guobin,Zhu, Wei,Ye, Haoyu,Yang, Shengyong,Luo, Youfu,Han, Jing,Yang, Jincheng,Li, Rui,Wei, Yuquan,Chen, Lijuan
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supporting information; experimental part
p. 4273 - 4278
(2010/09/04)
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- (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
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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
- 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.
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- Potent and selective aurora inhibitors identified by the expansion of a novel scaffold for protein kinase inhibition
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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
- 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
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p. 3080 - 3084
(2007/10/03)
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- SYNTHESIS OF N-2-CARBOXYETHYL-N-PHOSPHONOMETHYLGLYCINE
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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.
- Negrebetskii, Vad. V.,Kolesova, V. A.,Bobkova, R. G.,Chimishkyan, A. L.,Shvetsov-Shilovskii, N. I.
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p. 104 - 108
(2007/10/02)
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