吲哚美辛的正-碳硼烷衍生物作为环氧化酶（COX）-2 选择性抑制剂。
Ortho-carbaborane derivatives of indomethacin as cyclooxygenase (COX)-2 selective inhibitors.
机构信息
Institut für Anorganische Chemie der Universität Leipzig, Johannisallee 29, 04103 Leipzig, Germany.
出版信息
Bioorg Med Chem. 2012 Aug 1;20(15):4830-7. doi: 10.1016/j.bmc.2012.05.063. Epub 2012 Jun 5.
Abstract
A series of novel indomethacin analogues with carbaboranes as three-dimensional substitutes for the chlorophenyl ring have been prepared. Their cyclooxygenase (COX) inhibition and enzyme selectivity has been tested and compared to the corresponding adamantyl analogues. Surprisingly, only the ortho-carbaborane derivatives were active compounds. Preliminary biological studies gave an interesting insight into the validity of employing carbaboranes as pharmacophores.
摘要
已经制备了一系列新型吲哚美辛类似物，其中碳硼烷作为氯苯基环的三维取代物。已经测试了它们对环氧化酶（COX）的抑制作用和酶选择性，并与相应的金刚烷基类似物进行了比较。令人惊讶的是，只有邻位碳硼烷衍生物是活性化合物。初步的生物学研究深入了解了将碳硼烷用作药效团的有效性。
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