Non-thiol farnesyltransferase inhibitors: N-(4-acylamino-3-benzoylphenyl)-3-[5-(4-nitrophenyl)-2-furyl]acrylic acid amides
We have designed the nitrophenylfurylacryl-substituted benzophenone 4f as a non-thiol farnesyltransferase inhibitor utilizing a novel aryl binding site of farnesyltransferase. Variation of the 2-acylamino substituent at the benzophenone core structure of our initial lead 4f yielded several non-thiol...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry 2003-04, Vol.11 (7), p.1521-1530 |
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| container_issue | 7 |
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| container_title | Bioorganic & medicinal chemistry |
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| creator | KETTLER, Katja SAKOWSKI, Jacek SILBER, Katrin SATTLER, Isabel KLEBE, Gerhard SCHLITZER, Martin |
| description | We have designed the nitrophenylfurylacryl-substituted benzophenone 4f as a non-thiol farnesyltransferase inhibitor utilizing a novel aryl binding site of farnesyltransferase. Variation of the 2-acylamino substituent at the benzophenone core structure of our initial lead 4f yielded several non-thiol farnesyltransferase inhibitors with improved activity. These compounds display activity in the low nanomolar range. |
| doi_str_mv | 10.1016/S0968-0896(03)00064-6 |
| format | Article |
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Variation of the 2-acylamino substituent at the benzophenone core structure of our initial lead 4f yielded several non-thiol farnesyltransferase inhibitors with improved activity. These compounds display activity in the low nanomolar range.</description><identifier>ISSN: 0968-0896</identifier><identifier>EISSN: 1464-3391</identifier><identifier>DOI: 10.1016/S0968-0896(03)00064-6</identifier><identifier>PMID: 12705292</identifier><language>eng</language><publisher>Oxford: Elsevier Science</publisher><subject>Alkyl and Aryl Transferases - antagonists & inhibitors ; Amides - chemical synthesis ; Amides - pharmacology ; Antineoplastic agents ; Biological and medical sciences ; Enzyme Inhibitors - chemical synthesis ; Enzyme Inhibitors - pharmacology ; Farnesyltranstransferase ; Furans - chemical synthesis ; Furans - pharmacology ; General aspects ; Indicators and Reagents ; Magnetic Resonance Spectroscopy ; Medical sciences ; Models, Molecular ; Nitro Compounds - chemical synthesis ; Nitro Compounds - pharmacology ; Pharmacology. 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Variation of the 2-acylamino substituent at the benzophenone core structure of our initial lead 4f yielded several non-thiol farnesyltransferase inhibitors with improved activity. These compounds display activity in the low nanomolar range.</description><subject>Alkyl and Aryl Transferases - antagonists & inhibitors</subject><subject>Amides - chemical synthesis</subject><subject>Amides - pharmacology</subject><subject>Antineoplastic agents</subject><subject>Biological and medical sciences</subject><subject>Enzyme Inhibitors - chemical synthesis</subject><subject>Enzyme Inhibitors - pharmacology</subject><subject>Farnesyltranstransferase</subject><subject>Furans - chemical synthesis</subject><subject>Furans - pharmacology</subject><subject>General aspects</subject><subject>Indicators and Reagents</subject><subject>Magnetic Resonance Spectroscopy</subject><subject>Medical sciences</subject><subject>Models, Molecular</subject><subject>Nitro Compounds - chemical synthesis</subject><subject>Nitro Compounds - pharmacology</subject><subject>Pharmacology. 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Variation of the 2-acylamino substituent at the benzophenone core structure of our initial lead 4f yielded several non-thiol farnesyltransferase inhibitors with improved activity. These compounds display activity in the low nanomolar range.</abstract><cop>Oxford</cop><pub>Elsevier Science</pub><pmid>12705292</pmid><doi>10.1016/S0968-0896(03)00064-6</doi><tpages>10</tpages></addata></record> |
| fulltext | fulltext |
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| ispartof | Bioorganic & medicinal chemistry, 2003-04, Vol.11 (7), p.1521-1530 |
| issn | 0968-0896 1464-3391 |
| language | eng |
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| source | MEDLINE; ScienceDirect Journals (5 years ago - present) |
| subjects | Alkyl and Aryl Transferases - antagonists & inhibitors Amides - chemical synthesis Amides - pharmacology Antineoplastic agents Biological and medical sciences Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - pharmacology Farnesyltranstransferase Furans - chemical synthesis Furans - pharmacology General aspects Indicators and Reagents Magnetic Resonance Spectroscopy Medical sciences Models, Molecular Nitro Compounds - chemical synthesis Nitro Compounds - pharmacology Pharmacology. Drug treatments Protein Conformation Saccharomyces cerevisiae - enzymology Structure-Activity Relationship |
| title | Non-thiol farnesyltransferase inhibitors: N-(4-acylamino-3-benzoylphenyl)-3-[5-(4-nitrophenyl)-2-furyl]acrylic acid amides |
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