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

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

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

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Citation Number: 15

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 ...