Ortho-carbaborane derivatives of indomethacin as cyclooxygenase (COX)-2 selective inhibitors.
Authors
Scholz
M
Matthias
,
Blobaum
AL
Anna L
,
Marnett
LJ
Lawrence J
,
Hey-Hawkins
E
Evamarie
.
Bioorganic & medicinal chemistry. 2012 8 1; 20(15).
4830-7
Bioorganic & medicinal chemistry. 2012 8 1; 20(15).
4830-7
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.
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