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Efficient synthesis of 3-trifluoromethylphenyldiazirinyl oleic acid derivatives and Their biological activity for protein kinase C OAK
Hashimoto, Makoto; Nabeta, Kensuke; Murakami, Kentaro.
3-Trifluoromethylphenyldiazirine based oleic acids derivatives are synthesized to elucidate the functions of specific activation of protein kinase C (PKC) with oleic acid. The synthetic route is based on the alkylation of phenolic derivative with oleic acid equivalent and the post-functionalization. of the compound to achieve radiolabeling. Several compounds have biological activity for PKC with similar efficacy with that of oleic acid. The results indicated that the diaizinyl oleic acid derivatives should be useful to study the specific functions of oleic acid for PKC. (C) 2003 Elsevier Science Ltd. All rights reserved.
Palavras-chave: PHENYLALANINE; DIAZIRINE; RESPONSES; ANALOGS; PROBES.
Ano: 2003 URL: http://ir.obihiro.ac.jp/dspace/handle/10322/1324
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Simple method for the introduction of iodo-label on (3-trifluoromethyl) phenyldiazirine for photoaffinity labeling OAK
Hashimoto, Makoto; Kato, Yuhi; Hatanaka, Yasumaru.
A simple and mild method was developed for the introduction of iodo-label on (3-trifluoromethyl) phenyidiazirine (TPD) aromatic ring in the presence of three membered diazirine ring. An iodination protocol, I-2-BTI in CH3CN, was found to be effective even though affinity ligands are pre-installed.
Palavras-chave: HIGH SPECIFIC RADIOACTIVITY; CARBENE-GENERATING REAGENT; IODINATION METHOD; PROBES; DERIVATIVES; DIAZIRINE; EFFICIENT; ACID; PHOTOPHORE; PROTEINS.
Ano: 2006 URL: http://ir.obihiro.ac.jp/dspace/handle/10322/733
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