ortho-Carbaborane derivatives of indomethacin as cyclooxygenase (COX)-2 selective inhibitors

…, AL Blobaum, LJ Marnett, E Hey-Hawkins

文献索引：Scholz, Matthias; Blobaum, Anna L.; Marnett, Lawrence J.; Hey-Hawkins, Evamarie Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 15 p. 4830 - 4837

全文：HTML全文

被引用次数: 15

摘要

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 ...