Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 20, Issue 15, Pages 4830-4837Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2012.05.063
Keywords
Carbaborane; Carborane; Cyclooxygenase; Indomethacin; Nonsteroidal anti-inflammatory drugs
Funding
- Studienstiftung des Deutschen Volkes
- Graduate School of Excellence
- Deutsche Forschungsgemeinschaft
- National Institutes of Health [CA89450]
- Office Of Internatl Science &Engineering
- Office Of The Director [1157751] Funding Source: National Science Foundation
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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. (C) 2012 Elsevier Ltd. All rights reserved.
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