Preparation of S14161 and its analogues and the discovery of 6-bromo-8-ethoxy-3-nitro-2H-chromene as a more potent antitumor agent in vitro

…, K Han, B Cao, Z Zhang, X Du, LQ Tang, X Mao…

文献索引：Yin, Shu-Qiang; Shi, Min; Kong, Ting-Ting; Zhang, Cheng-Mei; Han, Kunkun; Cao, Biyin; Zhang, Zubin; Du, Xiaolin; Tang, Long-Qian; Mao, Xinliang; Liu, Zhao-Peng Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 11 p. 3314 - 3319

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被引用次数: 17

摘要

The small chemical compound 8-ethoxy-2-(4-fluorophenyl)-3-nitro-2H-chromene (S14161) was recently identified as an inhibitor of the phosphoinositide 3-kinase (PI3K). In the present study, we designed a novel synthesis of S14161 and prepared a series of its analogues via the oxa-Michael–Henry reaction in the presence of catalytic amounts of l-proline and triethylamine. Further structural simplification led to the identification of 6-bromo-8-ethoxy- ...