Ortho-carbaborane derivatives of indomethacin as cyclooxygenase (COX)-2 selective inhibitors期刊界 All Journals 搜尽天下杂志传播学术成果专业期刊搜索期刊信息化学术搜索

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Ortho-carbaborane derivatives of indomethacin as cyclooxygenase (COX)-2 selective inhibitors

Authors:	Scholz Matthias Blobaum Anna L Marnett Lawrence J Hey-Hawkins Evamarie

Institution:	1. Institut für Anorganische Chemie der Universität Leipzig, Johannisallee 29, 04103 Leipzig, Germany;2. A. B. Hancock Jr. Memorial Laboratory for Cancer Research, Department of Biochemistry, Vanderbilt Institute for Chemical Biology, Vanderbilt University School of Medicine, Nashville, TN 37232, USA;3. A. B. Hancock Jr. Memorial Laboratory for Cancer Research, Department of Chemistry, Vanderbilt Institute for Chemical Biology, Vanderbilt University School of Medicine, Nashville, TN 37232, USA;4. A. B. Hancock Jr. Memorial Laboratory for Cancer Research, Department of Pharmacology, Vanderbilt Institute for Chemical Biology, Vanderbilt University School of Medicine, Nashville, TN 37232, USA;5. Center in Molecular Toxicology, Vanderbilt-Ingram Cancer Center, Vanderbilt University School of Medicine, Nashville, TN 37232, USA

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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