Design, synthesis, and structure-activity relationship of new isobenzofuranone ligands of protein kinase C

Yoshiyasu Baba; Yosuke Ogoshi; Go Hirai; Takeshi Yanagisawa; Kumiko Nagamatsu; Satoshi Mayumi; Yuichi Hashimoto; Mikiko Sodeoka

doi:10.1016/j.bmcl.2004.02.097

Design, synthesis, and structure-activity relationship of new isobenzofuranone ligands of protein kinase C

Yoshiyasu Baba, Yosuke Ogoshi, Go Hirai, Takeshi Yanagisawa, Kumiko Nagamatsu, Satoshi Mayumi, Yuichi Hashimoto, Mikiko Sodeoka

Research output: Contribution to journal › Article

30 Citations (Scopus)

Abstract

Protein kinase C (PKC) is a family of enzymes, which play important roles in intracellular signal transduction. We have designed novel PKC ligands having an isobenzofuranone template, based on the proposed interaction of DAG (1,2-diacyl-sn-glycerol) with the PKCδ C1B ligand-binding domain. Several isobenzofuranone derivatives were synthesized and their PKCα binding activities were evaluated. The pivaloyl derivative 1f was found to be a strong PKCα ligand, and the structure-activity relationship is well explained by our proposed binding model.

Original language	English
Pages (from-to)	2963-2967
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	14
Issue number	11
DOIs	https://doi.org/10.1016/j.bmcl.2004.02.097
Publication status	Published - Jun 7 2004
Externally published	Yes

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All Science Journal Classification (ASJC) codes

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

Cite this

Baba, Y., Ogoshi, Y., Hirai, G., Yanagisawa, T., Nagamatsu, K., Mayumi, S., ... Sodeoka, M. (2004). Design, synthesis, and structure-activity relationship of new isobenzofuranone ligands of protein kinase C. Bioorganic and Medicinal Chemistry Letters, 14(11), 2963-2967. https://doi.org/10.1016/j.bmcl.2004.02.097

Design, synthesis, and structure-activity relationship of new isobenzofuranone ligands of protein kinase C. / Baba, Yoshiyasu; Ogoshi, Yosuke; Hirai, Go; Yanagisawa, Takeshi; Nagamatsu, Kumiko; Mayumi, Satoshi; Hashimoto, Yuichi; Sodeoka, Mikiko.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 14, No. 11, 07.06.2004, p. 2963-2967.

Research output: Contribution to journal › Article

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10.1016/j.bmcl.2004.02.097