PubMed:2153828 JSONTXT

{"target":"http://pubannotation.org/docs/sourcedb/PubMed/sourceid/2153828","sourcedb":"PubMed","sourceid":"2153828","source_url":"http://www.ncbi.nlm.nih.gov/pubmed/2153828","text":"1,4-Dihydronaphthoquinones, hydroindoloquinones, benzofurans, and benzothiophenes as inhibitors of 5-lipoxygenase. Synthesis and structure-activity studies.\nA series of substituted 1,4-dihydronaphthoquinones, hydroindoloquinones, benzofuran-4,7-dihydroquinones, and benzothiophene-4,7-dihydroquinones were synthesized and evaluated for inhibitory activity against 5-lipoxygenase. These compounds were found to be active in vitro for LTC4/D4 inhibition with the potencies (IC50's) ranging from 0.2 to 85 microM. Active 1,4-dihydronaphthoquinone acetates (IC50 less than 20 microM) were evaluated in an ex vivo LTB4 inhibition assay. The acetates of 1,4-dihydronaphthoquinones containing the alkyl substituent(s) (2-n-butyl, 11, and 2,3-diethyl, 15) exhibited the best activity in LTC4/D4 inhibition (IC50 = 0.2-0.4 microM, in vitro) as well as in LTB4 inhibition (60-75% inhibition).","tracks":[{"project":"SCAI-Test","denotations":[{"id":"T1","span":{"begin":181,"end":207},"obj":"CHED"},{"id":"T2","span":{"begin":209,"end":228},"obj":"CHED"},{"id":"T3","span":{"begin":230,"end":260},"obj":"CHED"},{"id":"T4","span":{"begin":266,"end":300},"obj":"CHED"},{"id":"T5","span":{"begin":518,"end":552},"obj":"CHED"},{"id":"T6","span":{"begin":636,"end":644},"obj":"CHED"},{"id":"T7","span":{"begin":648,"end":674},"obj":"CHED"},{"id":"T8","span":{"begin":690,"end":695},"obj":"CHED"},{"id":"T9","span":{"begin":712,"end":721},"obj":"CHED"},{"id":"T10","span":{"begin":731,"end":742},"obj":"CHED"}],"attributes":[{"subj":"T1","pred":"source","obj":"SCAI-Test"},{"subj":"T2","pred":"source","obj":"SCAI-Test"},{"subj":"T3","pred":"source","obj":"SCAI-Test"},{"subj":"T4","pred":"source","obj":"SCAI-Test"},{"subj":"T5","pred":"source","obj":"SCAI-Test"},{"subj":"T6","pred":"source","obj":"SCAI-Test"},{"subj":"T7","pred":"source","obj":"SCAI-Test"},{"subj":"T8","pred":"source","obj":"SCAI-Test"},{"subj":"T9","pred":"source","obj":"SCAI-Test"},{"subj":"T10","pred":"source","obj":"SCAI-Test"}]}],"config":{"attribute types":[{"pred":"source","value type":"selection","values":[{"id":"SCAI-Test","color":"#b9ec93","default":true}]}]}}