Asymmetric synthesis of isobenzofuranone derivatives and their unique character as protein kinase Cα (PKCα) activators

Go Hirai, Yosuke Ogoshi, Megumi Ohkubo, Yuki Tamura, Toru Watanabe, Tadashi Shimizu, Mikiko Sodeoka

研究成果: Contribution to journalArticle

5 引用 (Scopus)

抜粋

Efficient enantio-selective synthesis of conformationally constrained diacylglycerol analogues, 7-substituted isobenzofuranone derivatives, originally developed by us as PKCα ligands, was achieved by asymmetric dihydroxylation and γ-lactone formation via ortho-lithiation and carboxylation. A series of derivatives having straight and/or branched side chains were synthesized and evaluated, and low-nanomolar-concentration affinity ligands and highly potent PKCα activators were found among them. These potent ligands induced phenotypic change of K562 cells, which is characteristic of PKC activators.

元の言語英語
ページ(範囲)3609-3612
ページ数4
ジャーナルTetrahedron Letters
50
発行部数26
DOI
出版物ステータス出版済み - 7 1 2009
外部発表Yes

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Drug Discovery
  • Organic Chemistry

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