title: Ortho-carbaborane derivatives of indomethacin as cyclooxygenase (COX)-2 selective inhibitors.
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.
authors: Institut für Anorganische Chemie der Universität Leipzig, Johannisallee 29, 04103 Leipzig, Germany.
authors: Matthias
authors: M
authors: Scholz
authors: Anna L
authors: AL
authors: Blobaum
authors: Lawrence J
authors: LJ
authors: Marnett
authors: Evamarie
authors: E
authors: Hey-Hawkins
mesh_terms: D001880:Boranes / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D051546:Cyclooxygenase 2 / Q000378:metabolism*; D052246:Cyclooxygenase 2 Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D007213:Indomethacin / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D008958:Models, Molecular; D015394:Molecular Structure; D013329:Structure-Activity Relationship
chemical_list: D001880:Boranes; D052246:Cyclooxygenase 2 Inhibitors; D051546:Cyclooxygenase 2; D007213:Indomethacin