Design and in Vitro Activities of N-Alkyl-N-[(8-R-2, 2-dimethyl-2 H-chromen-6-yl) methyl] heteroarylsulfonamides, Novel, Small-Molecule Hypoxia Inducible Factor-1 …

…, C Tan, D Culver, JP Snyder, EG Van Meir…

文献索引：Mun, Jiyoung; Jabbar, Adnan Abdul; Devi, Narra Sarojini; Yin, Shaoman; Wang, Yingzhe; Tan, Chalet; Culver, Deborah; Snyder, James P.; Van Meir, Erwin G.; Goodman, Mark M. Journal of Medicinal Chemistry, 2012 , vol. 55, # 15 p. 6738 - 6750

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被引用次数: 21

摘要

The hypoxia inducible factor (HIF) pathway is an attractive target for cancer, as it controls tumor adaptation to growth under hypoxia and mediates chemotherapy and radiation resistance. We previously discovered 3, 4-dimethoxy-N-[(2, 2-dimethyl-2 H-chromen-6-yl) methyl]-N-phenylbenzenesulfonamide as a novel, small-molecule HIF-1 pathway inhibitor in a high-throughput cell-based assay, but its in vivo delivery is hampered by poor aqueous ...