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Non-thiol farnesyltransferase inhibitors: N-(4-acylamino-3-benzoylphenyl)-3-[5-(4-nitrophenyl)-2-furyl]acrylic acid amides |
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| Authors: | Kettler Katja Sakowski Jacek Silber Katrin Sattler Isabel Klebe Gerhard Schlitzer Martin |
| Affiliation: | 1. Beijing National Laboratory for Molecular Sciences, Radiochemistry and Radiation Chemistry Key Laboratory of Fundamental Science, The Key Laboratory of Polymer Chemistry and Physics of the Ministry of Education, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China;2. Fujian Key Laboratory of Architectural Coating, Skshu Paint Co., Ltd., 518 North Liyuan Avenue, Licheng District, Putian, Fujian 351100, China;3. Institute of Chemical Defense, Beijing 100191, China;4. School of Materials Design & Engineering, Beijing Institute of Fashion Technology, Beijing 100029, China |
| Abstract: | 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. |
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