排序方式: 共有5条查询结果,搜索用时 15 毫秒
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R A Smith A Bhargava C Browe J Chen J Dumas H Hatoum-Mokdad R Romero 《Bioorganic & medicinal chemistry letters》2001,11(22):2951-2954
Peptidomimetic aminomethyl ketones have been identified as a new class of cathepsin K inhibitors. Traditional and high-speed parallel synthesis techniques were applied to investigate this series. Structure-activity relationships were established, and certain analogues were characterized with IC(50) values in the range 200-500 nM. 相似文献
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Dumas J Hatoum-Mokdad H Sibley RN Smith RA Scott WJ Khire U Lee W Wood J Wolanin D Cooley J Bankston D Redman AM Schoenleber R Caringal Y Gunn D Romero R Osterhout M Paulsen H Housley TJ Wilhelm SM Pirro J Chien DS Ranges GE Shrikhande A Muzsi A Bortolon E Wakefield J Gianpaolo Ostravage C Bhargava A Chau T 《Bioorganic & medicinal chemistry letters》2002,12(12):1559-1562
Inhibitors of the MAP kinase p38 provide a novel approach for the treatment of osteoporosis, inflammatory disorders, and cancer. We have identified N-(3-tert-butyl-1-methyl-5-pyrazolyl)-N'-(4-(4-pyridinylmethyl)phenyl)urea as a potent and selective p38 kinase inhibitor in biochemical and cellular assays. This compound is orally active in two acute models of cytokine release (TNF-induced IL-6 and LPS-induced TNF) and a chronic model of arthritis (20-day murine collagen-induced arthritis). 相似文献
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Dumas J Hatoum-Mokdad H Sibley R Riedl B Scott WJ Monahan MK Lowinger TB Brennan C Natero R Turner T Johnson JS Schoenleber R Bhargava A Wilhelm SM Housley TJ Ranges GE Shrikhande A 《Bioorganic & medicinal chemistry letters》2000,10(18):2051-2054
Inhibitors of the MAP kinase p38 are potentially useful for the treatment of arthritis and osteoporosis. Several 2,3-dichlorophenyl ureas were identified as small-molecule inhibitors of p38 by a combinatorial chemistry effort. Optimization for cellular potency led to the discovery of a new class of potent and selective p38 kinase inhibitors, exemplified by the 1-phenyl-5-pyrazolyl urea 7 (IC50 = 13 nM). 相似文献
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Sibley R Hatoum-Mokdad H Schoenleber R Musza L Stirtan W Marrero D Carley W Xiao H Dumas J 《Bioorganic & medicinal chemistry letters》2003,13(11):1919-1922
Three synthetic routes towards a novel estrogen receptor ligand template based on a rigid bicyclo-[3.3.1]-nonene core have been investigated. The prototype compound exhibits potent binding at the ERbeta receptor and promising estrogen receptor subtype selectivity. 相似文献
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J Dumas D Brittelli J Chen B Dixon H Hatoum-Mokdad G K?nig R Sibley J Witowsky S Wong 《Bioorganic & medicinal chemistry letters》1999,9(17):2531-2536
Cathepsin D, a lysosomal aspartyl protease, has been implicated in the pathology of Alzheimer's disease as well as breast and ovarian cancer. A weakly active cathepsin D inhibitor was identified by high throughput screening. Subsequent optimization led to the discovery of a new class of small molecule inhibitors of this enzyme, culminating with the sulfonamide 13 (IC50 = 250 nM). 相似文献
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