943230-33-9Relevant academic research and scientific papers
Chiral 6-aryl-furo[2,3-d]pyrimidin-4-amines as EGFR inhibitors
Han, Jin,Kaspersen, Svein Jacob,Nervik, Sondre,N?rsett, Kristin G.,Sundby, Eirik,Hoff, B?rd Helge
, p. 278 - 299 (2016/06/14)
Epidermal growth factor receptor inhibitors are of importance in cancer therapy and possibly in the management of pain. Herein, we report a structure-activity relationship study with 29 new 6-aryl-furo[2,3-d]pyrimidin-4-amines, involving modification of the 4-amino group and 6-aryl function. The EGFR activity was especially dependent on having a chiral 4-benzylamino group with correct stereochemistry. Molecular dynamics indicate this to be due to favourable cation-π interactions. The most active inhibitor identified, equipotent to Erlotinib, was substituted with (R)-1-phenylethylamine at C-4 and a N1, N1-dimethyl-1,2-diamine group in para position of the 6-aryl moiety. These new furopyrimidines had a different off-target kinase profile when compared to Erlotinib, and also possessed high activity towards Ba/F3 EGFRL858R reporter cells. Further, comparing the EGFR data of the furo[2,3-d]pyrimidin-4-amines with that of the corresponding thieno- and pyrrolopyrimidines concludes the furopyrimidine scaffold to be highly useful for development of new epidermal growth factor receptor antagonists.
SUBSTITUTED 4-(SELENOPHEN-2(OR-3)-YLAMINO)PYRIMIDINE COMPOUNDS AND METHODS OF USE THEREOF
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, (2013/10/22)
Selenophene compounds of formula (I) are described herein. In the compounds of Formula (I), ring A is a 6-membered aromatic fused ring, optionally containing one, two or three nitrogen atoms; a 5-membered heteroaromatic fused ring; or a mono- or bicyclic
Novel, Cyclically Substituted Furopyrimidine Derivatives and Use Thereof
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, (2011/06/19)
The present application relates to novel, cyclically substituted furopyrimidine derivatives, methods for their production, their use for the treatment and/or prophylaxis of diseases and their use for the production of medicinal products for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular diseases.
SUBSTITUTED FUROPYRIMIDINES AND USE THEREOF
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, (2011/07/29)
The present application relates to novel substituted furopyrimidine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular diseases.
Fused Bicyclic and Tricyclic Pyrimidine Compounds as Tyrosine Kinase Inhibitors
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Page/Page column 49, (2010/06/11)
Fused bicyclic or tricyclic compounds of formula (I): wherein A, B, C, X, Y, m, and n are defined herein. Also disclosed are a method for inhibiting EGFR kinase activity and a method for treating cancer with these compounds.
Identification, SAR studies, and X-ray Co-crystallographic analysis of a novel furanopyrimidine aurora kinase a inhibitor
Coumar, Mohane Selvaraj,Tsai, Ming-Tsung,Chu, Chang-Ying,Uang, Biing-Jiun,Lin, Wen-Hsing,Chang, Chun-Yu,Chang, Teng-Yuan,Leou, Jiun-Shyang,Teng, Chi-Huang,Wu, Jian-Sung,Fang, Ming-Yu,Chen, Chun-Hwa,Hsu, John T.-A.,Wu, Su-Ying,Chao, Yu-Sheng,Hsieh, Hsing-Pang
experimental part, p. 255 - 267 (2010/12/18)
Herein we reveal a simple method for the identification of novel Aurora kinase A inhibitors through substructure searching of an in-house compound library to select compounds for testing. A hydrazone fragment conferring Aurora kinase activity and heterocy
Novel, Acyclically Substituted Furopyrimidine Derivatives and Use Thereof
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Page/Page column 10; 19-20, (2009/12/28)
The present application relates to novel, acyclically substituted furopyrimidine derivatives, methods for their production, their use for the treatment and/or prophylaxis of diseases and their use for the production of medicinal products for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular diseases.
