• Scholz M, Blobaum AL, Marnett LJ, Hey-Hawkins E. Ortho-carbaborane derivatives of indomethacin as cyclooxygenase (COX)-2 selective inhibitors. Bioorganic & medicinal chemistry. 2012 Aug 1;20(15). 4830-7. PMID: 22748709 [PubMed]. PMCID: PMC3408963. NIHMSID: NIHMS382872.


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.

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