文章基本信息

标题：Modulators of Tumor Necrosis Factor α Production Bearing Dicarba-closo-dodecaborane as a Hydrophobic Pharmacophore
本地全文：下载
作者：Motonori TSUJI ; Yukiko KOISO ; Hiroyasu TAKAHASHI 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2000
卷号：23
期号：4
页码：513-516
DOI：10.1248/bpb.23.513
出版社：The Pharmaceutical Society of Japan
摘要：Previous studies on the structural development of tumor necrosis factor α (TNF-α) production regulators derived from thalidomide (N-α-phthalimidoglutarimide) revealed that a hydrophobic substituent at the nitrogen atom of the phathalimide ring is critical for potent activity. We have designed and pepared phthalimide derivatives bearing a boron cluster, dicarba-closo-dodecaborane (carborane), which has a hydrophobic character and spherical geometry, as a novel candidate of biological response modifiers. These compounds were shown to regulate TNF-α production by HL-60 cells, as expected. The result provides a further example of the application of carborane as a hydrophobic pharmacophore of biologically active molecules.
关键词：dicarba-closo-dodecaborane;tumor necrosis factor α;HL-60;phorbol ester;okadaic acid