Formylchromone derivatives as a novel class of protein tyrosine phosphatase 1B inhibitors

Yi Sup Shim; Ki Chul Kim; Dae Yoon Chi; Keun Hyeung Lee; Hyeongjin Cho

doi:10.1016/S0960-894X(03)00479-7

Formylchromone derivatives as a novel class of protein tyrosine phosphatase 1B inhibitors

Yi Sup Shim, Ki Chul Kim, Dae Yoon Chi, Keun Hyeung Lee, Hyeongjin Cho

Inha University

Research output: Contribution to journal › Article › peer-review

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Abstract

Formylchromone inhibits a human protein tyrosine phosphatase PTP1B with a IC₅₀ value of 73 μM. The chemical reactivity of formylchromone was adjusted by substitution at various positions of the formylchromone skeleton. In an initial assessment of the structure-activity relationship, the most potent inhibitor showed an IC₅₀ of 4.3 μM against PTP1B and strong or medium selectivity against other human PTPases, LAR and TC-PTP. This compound, however, was not selective against microbial PTPases, YPTP1 and YOP. The potency and selectivity of the formylchromone derivatives expecting further improvements provides a novel pharmacophore for the design of drugs for the treatmenrt of type 2 diabetes and obesity.

Original language	English
Pages (from-to)	2561-2563
Number of pages	3
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	13
Issue number	15
DOIs	https://doi.org/10.1016/S0960-894X(03)00479-7
State	Published - 4 Aug 2003

Bibliographical note

Funding Information:
This work was supported by the grant (R05-2001-000-00551-0) from the Basic Research Program of the Korea Science & Engineering Foundation.

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title = "Formylchromone derivatives as a novel class of protein tyrosine phosphatase 1B inhibitors",

abstract = "Formylchromone inhibits a human protein tyrosine phosphatase PTP1B with a IC50 value of 73 μM. The chemical reactivity of formylchromone was adjusted by substitution at various positions of the formylchromone skeleton. In an initial assessment of the structure-activity relationship, the most potent inhibitor showed an IC50 of 4.3 μM against PTP1B and strong or medium selectivity against other human PTPases, LAR and TC-PTP. This compound, however, was not selective against microbial PTPases, YPTP1 and YOP. The potency and selectivity of the formylchromone derivatives expecting further improvements provides a novel pharmacophore for the design of drugs for the treatmenrt of type 2 diabetes and obesity.",

author = "Shim, {Yi Sup} and Kim, {Ki Chul} and Chi, {Dae Yoon} and Lee, {Keun Hyeung} and Hyeongjin Cho",

note = "Funding Information: This work was supported by the grant (R05-2001-000-00551-0) from the Basic Research Program of the Korea Science & Engineering Foundation. ",

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doi = "10.1016/S0960-894X(03)00479-7",

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T1 - Formylchromone derivatives as a novel class of protein tyrosine phosphatase 1B inhibitors

AU - Shim, Yi Sup

AU - Kim, Ki Chul

AU - Chi, Dae Yoon

AU - Lee, Keun Hyeung

AU - Cho, Hyeongjin

N1 - Funding Information: This work was supported by the grant (R05-2001-000-00551-0) from the Basic Research Program of the Korea Science & Engineering Foundation.

PY - 2003/8/4

Y1 - 2003/8/4

N2 - Formylchromone inhibits a human protein tyrosine phosphatase PTP1B with a IC50 value of 73 μM. The chemical reactivity of formylchromone was adjusted by substitution at various positions of the formylchromone skeleton. In an initial assessment of the structure-activity relationship, the most potent inhibitor showed an IC50 of 4.3 μM against PTP1B and strong or medium selectivity against other human PTPases, LAR and TC-PTP. This compound, however, was not selective against microbial PTPases, YPTP1 and YOP. The potency and selectivity of the formylchromone derivatives expecting further improvements provides a novel pharmacophore for the design of drugs for the treatmenrt of type 2 diabetes and obesity.

AB - Formylchromone inhibits a human protein tyrosine phosphatase PTP1B with a IC50 value of 73 μM. The chemical reactivity of formylchromone was adjusted by substitution at various positions of the formylchromone skeleton. In an initial assessment of the structure-activity relationship, the most potent inhibitor showed an IC50 of 4.3 μM against PTP1B and strong or medium selectivity against other human PTPases, LAR and TC-PTP. This compound, however, was not selective against microbial PTPases, YPTP1 and YOP. The potency and selectivity of the formylchromone derivatives expecting further improvements provides a novel pharmacophore for the design of drugs for the treatmenrt of type 2 diabetes and obesity.

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Formylchromone derivatives as a novel class of protein tyrosine phosphatase 1B inhibitors

Abstract

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