Efficient synthesis of 3-trifluoromethylphenyldiazirinyl oleic acid derivatives and their biological activity for protein kinase C.
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.
Hashimoto
Makoto
M
Department of Bioresource Science, Obihiro University of Agriculture and Veterinary Medicine, Inada-cho, Obihiro 080-8555, Hokkaido, Japan. hasimoto@obihiro.ac.jp
Nabeta
Kensuke
K
Murakami
Kentaro
K
D001388:Aziridines / Q000138:chemical synthesis* / Q000494:pharmacology; D020536:Enzyme Activators / Q000138:chemical synthesis* / Q000737:chemistry; D006801:Humans; D009829:Oleic Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D019920:Photoaffinity Labels / Q000138:chemical synthesis* / Q000737:chemistry; D011493:Protein Kinase C / Q000737:chemistry*; D011994:Recombinant Proteins / Q000737:chemistry; D013329:Structure-Activity Relationship
C479981:3-trifluoromethylphenyldiazirinyl oleic acid; D001388:Aziridines; D020536:Enzyme Activators; D009829:Oleic Acids; D019920:Photoaffinity Labels; D011994:Recombinant Proteins; D011493:Protein Kinase C