期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 19, 期 10, 页码 3242-3248出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2011.03.054
关键词
Carborane; Carbaborane; Cyclooxygenase; Indomethacin; Nonsteroidal anti-inflammatory drugs
资金
- Studienstiftung des Deutschen Volkes
- Deutsche Forschungsgemeinschaft
- National Institutes of Health [CA89450]
- Office Of Internatl Science &Engineering
- Office Of The Director [1157751] Funding Source: National Science Foundation
Nonsteroidal anti-inflammatory drugs (NSAIDs) exert their pharmacological activities by inhibiting cyclooxygenase (COX)-1 and COX-2. Previous studies have shown that esters and amides of nonselective inhibitors such as indomethacin are selective against COX-2, which is the therapeutically relevant isoform. Structure-activity analysis indicates that substituted phenyl rings are tolerated as ester components. In the present study, the introduction of inorganic ortho-and meta-carbaborane moieties was explored with the aim to create COX-2 inhibitors and more importantly to investigate the validity of using these boron clusters as drug entities. Interestingly, only the ortho-carbaborane ester was active whereas the meta isomer was not. A similar lack of inhibitory potency was observed when an adamantyl substituent or alkylene spacers at the carbaborane were introduced in the ester functionality. (C) 2011 Elsevier Ltd. All rights reserved.
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