On July 8, 2010, Coumar, Mohane Selvaraj; Chu, Chang-Ying; Lin, Cheng-Wei; Shiao, Hui-Yi; Ho, Yun-Lung; Reddy, Randheer; Lin, Wen-Hsing; Chen, Chun-Hwa; Peng, Yi-Hui; Leou, Jiun-Shyang; Lien, Tzu-Wen; Huang, Chin-Ting; Fang, Ming-Yu; Wu, Szu-Huei; Wu, Jian-Sung; Chittimalla, Santhosh Kumar; Song, Jen-Shin; Hsu, John T.-A.; Wu, Su-Ying; Liao, Chun-Chen; Chao, Yu-Sheng; Hsieh, Hsing-Pang published an article.COA of Formula: C4H8ClNOS The title of the article was Fast-Forwarding Hit to Lead: Aurora and Epidermal Growth Factor Receptor Kinase Inhibitor Lead Identification. And the article contained the following:
Furanopyrimidines such as I [R = (S)-HOCH2CHPh; R1 = 3-(H2C:CCONH)C6H4] are prepared as Aurora A kinase and epidermal growth factor receptor (EGFR) inhibitors by preparation of a combinatorial library of approx. 350 furanopyridines and optimization of the inhibitors found from the library. The initial hit compound I (R = HOCH2CH2; R1 = Ph) was modified to better fit the back pocket to produce the potent Aurora A kinase inhibitor I (R = 4-PhNHCONHC6H4; R1 = Ph) with submicromolar antiproliferative activity in the HCT-116 human colon cancer cell line. On the basis of docking studies with EGFR hit I [R = (S)-HOCH2CHPh; R1 = Ph], introduction of an acrylamide Michael acceptor group led to I [R = (S)-HOCH2CHPh; R1 = 3-(H2C:CCONH)C6H4], which inhibited both the wild and mutant EGFR kinases and also showed antiproliferative activity in the gefitinib-resistant HCC827 human lung cancer cells. The X-ray cocrystal structures of I (R = HOCH2CH2, 4-PhNHCONHC6H4; R1 = Ph) bound to Aurora A kinase and the crystal structure of I [R = (S)-HOCH2CHPh; R1 = 3-(H2C:CCONH)C6H4] bound to EGFR confirmed their hypothesized binding modes. The experimental process involved the reaction of 3-Aminodihydrothiophen-2(3H)-one hydrochloride(cas: 6038-19-3).COA of Formula: C4H8ClNOS
The Article related to furanopyrimidine combinatorial library preparation aurora egfr kinase inhibitor, structure furanopyrimidine activity aurora egfr kinase inhibitor, optimization furanopyrimidine aurora egfr kinase inhibitor activity, mol crystal structure furanopyrimidine bound aurora egfr kinase and other aspects.COA of Formula: C4H8ClNOS
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