期刊
CHEMMEDCHEM
卷 8, 期 2, 页码 329-335出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.201200455
关键词
carbaboranes; carboranes; COX; heterocycles; inhibitors; McMurry
资金
- Fonds der Chemischen Industrie
- Studienstiftung des Deutschen Volkes
- Graduate School Building with Molecules and Nano-objects (BuildMoNa)
- Deutsche Forschungsgemeinschaft
- National Institutes of Health [CA89450]
- Office Of The Director
- Office Of Internatl Science &Engineering [1157751] Funding Source: National Science Foundation
Cyclooxygenase-2 (COX-2) inhibitors have been the focus of medicinal chemistry efforts for years, and many compounds that exhibit high selectivity and affinity have been developed. As carbaboranes represent interesting pharmacophores as phenyl mimetics in drug development, this paper presents the synthesis of carbaboranyl derivatives of COX-2-selective 2,3-disubstituted indoles. Despite the lability of carbaboranes under reducing conditions, 2-carbaborane-3-phenyl-1H-indoles could be synthesized by McMurry cyclization of the corresponding amides. Whereas the meta-carbaboranyl-substituted derivatives lacked COX inhibitory activity, an ortho-carbaboranyl analogue was active, but showed a selectivity shift toward COX-1.
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