833451-03-9Relevant academic research and scientific papers
An efficient synthesis of 4,6-substituted pyrrolo[3,2-d]pyrimidines by silver-catalyzed cyclization of acetylene amine
Xie, Rui,Hu, Ying,Wan, Huixin,Hu, Yanwei,Chen, Shaohua,Zhang, Shilei,Zhang, Yinan
supporting information, p. 2418 - 2421 (2016/05/19)
A silver catalyzed cyclization of acetylene amine was developed to synthesize 4,6-substituted pyrrolo[3,2-d]pyrimidine, a bioactive isosteric scaffold of purine. Starting from simple commercially available acetylenes and pyrimidines, the method was found
Tricyclic azepine derivatives: Pyrimido[4,5-b]-1,4-benzoxazepines as a novel class of epidermal growth factor receptor kinase inhibitors
Smith II, Leon,Piatnitski, Evgueni L.,Kiselyov, Alexander S.,Ouyang, Xiaohu,Chen, Xiaoling,Burdzovic-Wizemann, Sabina,Xu, Yongjiang,Wang, Ying,Rosler, Robin L.,Patel, Sheetal N.,Chiang, Hui-Hsien,Milligan, Daniel L.,Columbus, John,Wong, Wai C.,Doody, Jacqueline F.,Hadari, Yaron R.
, p. 1643 - 1646 (2007/10/03)
A novel class of pyrimido[4,5-b]-1,4-benzoxazepines is described as inhibitors of epidermal growth factor receptor (EGFR) tyrosine kinase. Two compounds display potent EGFR inhibitory activity of less than 1 μM in cellular phosphorylation assays (IC50 0.47-0.69 μM) and are highly selective against a small kinase panel. Such compounds demonstrate anti-EGFR activity within a class that is different from any known EGFR inhibitor scaffolds. They also provide a basis for the design of kinase inhibitors with the desired selectivity profile.
Novel tricyclic azepine derivatives: Biological evaluation of pyrimido[4,5-b]-1,4-benzoxazepines, thiazepines, and diazepines as inhibitors of the epidermal growth factor receptor tyrosine kinase
Smith II, Leon,Wong, Wai C.,Kiselyov, Alexander S.,Burdzovic-Wizemann, Sabina,Mao, Yunyu,Xu, Yongjiang,Duncton, Matthew A.J.,Kim, Ki,Piatnitski, Evgueni L.,Doody, Jacqueline F.,Wang, Ying,Rosler, Robin L.,Milligan, Daniel,Columbus, John,Balagtas, Chris,Lee, Sui Ping,Konovalov, Andrey,Hadari, Yaron R.
, p. 5102 - 5106 (2007/10/03)
Novel tricyclic derivatives containing an oxazepine, thiazepine, or diazepine ring were studied for their EGFR tyrosine kinase inhibitory activity. While the oxazepines were in general more potent than thiazepines, the diazepines displayed somewhat differ
