Synthesis of miltirone analogues as inhibitors of Cdc25 phosphatases

Weigang Huang; Jingya Li; Wei Zhang; Yueyang Zhou; Chuanming Xie; Yu Luo; Yunfei Li; Jingli Wang; Jia Li; Wei Lu

doi:10.1016/j.bmcl.2005.12.080

Synthesis of miltirone analogues as inhibitors of Cdc25 phosphatases

Weigang Huang
, Jingya Li^*
, Wei Zhang
, Yueyang Zhou
, Chuanming Xie
, Yu Luo
, Yunfei Li
, Jingli Wang
, Jia Li^*
, Wei Lu

^*Corresponding author for this work

School of Chemistry and Molecular Engineering

CAS - Shanghai Institute of Materia Medica
East China Normal University

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

37 Scopus citations

Abstract

Miltirone analogues were synthesized and evaluated for inhibitory activity against Cdc25 and PTP1B. Most of the compounds demonstrated potent Cdc25 inhibitory activity, and several exhibited higher selectivity for Cdc25 than for PTP1B. In a cytotoxic assay, most of the compounds displayed cytotoxicity against the tumor cell lines A549 and HCT-116, producing IC₅₀ values in the micromolar range.

Original language	English
Pages (from-to)	1905-1908
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	16
Issue number	7
DOIs	https://doi.org/10.1016/j.bmcl.2005.12.080
State	Published - 1 Apr 2006

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

Cancer
Cdc25 phosphatases
Miltirone

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10.1016/j.bmcl.2005.12.080

Cite this

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title = "Synthesis of miltirone analogues as inhibitors of Cdc25 phosphatases",

abstract = "Miltirone analogues were synthesized and evaluated for inhibitory activity against Cdc25 and PTP1B. Most of the compounds demonstrated potent Cdc25 inhibitory activity, and several exhibited higher selectivity for Cdc25 than for PTP1B. In a cytotoxic assay, most of the compounds displayed cytotoxicity against the tumor cell lines A549 and HCT-116, producing IC50 values in the micromolar range.",

keywords = "Cancer, Cdc25 phosphatases, Miltirone",

author = "Weigang Huang and Jingya Li and Wei Zhang and Yueyang Zhou and Chuanming Xie and Yu Luo and Yunfei Li and Jingli Wang and Jia Li and Wei Lu",

year = "2006",

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doi = "10.1016/j.bmcl.2005.12.080",

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TY - JOUR

T1 - Synthesis of miltirone analogues as inhibitors of Cdc25 phosphatases

AU - Huang, Weigang

AU - Li, Jingya

AU - Zhang, Wei

AU - Zhou, Yueyang

AU - Xie, Chuanming

AU - Luo, Yu

AU - Li, Yunfei

AU - Wang, Jingli

AU - Li, Jia

AU - Lu, Wei

PY - 2006/4/1

Y1 - 2006/4/1

N2 - Miltirone analogues were synthesized and evaluated for inhibitory activity against Cdc25 and PTP1B. Most of the compounds demonstrated potent Cdc25 inhibitory activity, and several exhibited higher selectivity for Cdc25 than for PTP1B. In a cytotoxic assay, most of the compounds displayed cytotoxicity against the tumor cell lines A549 and HCT-116, producing IC50 values in the micromolar range.

AB - Miltirone analogues were synthesized and evaluated for inhibitory activity against Cdc25 and PTP1B. Most of the compounds demonstrated potent Cdc25 inhibitory activity, and several exhibited higher selectivity for Cdc25 than for PTP1B. In a cytotoxic assay, most of the compounds displayed cytotoxicity against the tumor cell lines A549 and HCT-116, producing IC50 values in the micromolar range.

KW - Cancer

KW - Cdc25 phosphatases

KW - Miltirone

UR - https://www.scopus.com/pages/publications/33144467432

U2 - 10.1016/j.bmcl.2005.12.080

DO - 10.1016/j.bmcl.2005.12.080

M3 - 文章

C2 - 16434190

AN - SCOPUS:33144467432

SN - 0960-894X

VL - 16

SP - 1905

EP - 1908

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 7

ER -

Synthesis of miltirone analogues as inhibitors of Cdc25 phosphatases

Abstract

UN SDGs

Keywords

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