The discovery of colchicine-SAHA hybrids as a new class of antitumor agents

Xuan Zhang; Jie Zhang; Linjiang Tong; Yu Luo; Mingbo Su; Yi Zang; Jia Li; Wei Lu; Yi Chen

doi:10.1016/j.bmc.2013.03.049

The discovery of colchicine-SAHA hybrids as a new class of antitumor agents

Xuan Zhang
, Jie Zhang
, Linjiang Tong
, Yu Luo
, Mingbo Su
, Yi Zang
, Jia Li
, Wei Lu^*
, Yi Chen

^*Corresponding author for this work

School of Chemistry and Molecular Engineering

East China Normal University
CAS - Shanghai Institute of Materia Medica

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

71 Scopus citations

Abstract

A novel class of colchicine-SAHA hybrids were designed and synthesised based on the synergistic antitumor effect of tubulin inhibitors and histone deacetylases (HDAC) inhibitors. To the best of our knowledge, this is the first design of molecules that are dual inhibitors of tubulin and HDAC. Biological evaluations of these compounds included the inhibitory activity of HDAC, in vitro cell cycle analysis in BEL-7402 cells as well as cytotoxicity in five cancer cell lines.

Original language	English
Pages (from-to)	3240-3244
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry
Volume	21
Issue number	11
DOIs	https://doi.org/10.1016/j.bmc.2013.03.049
State	Published - 1 Jun 2013

UN SDGs

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

SDG 3 Good Health and Well-being

Keywords

Colchicine
HDAC
Hybrid
SAHA
Tubulin

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10.1016/j.bmc.2013.03.049

Cite this

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title = "The discovery of colchicine-SAHA hybrids as a new class of antitumor agents",

abstract = "A novel class of colchicine-SAHA hybrids were designed and synthesised based on the synergistic antitumor effect of tubulin inhibitors and histone deacetylases (HDAC) inhibitors. To the best of our knowledge, this is the first design of molecules that are dual inhibitors of tubulin and HDAC. Biological evaluations of these compounds included the inhibitory activity of HDAC, in vitro cell cycle analysis in BEL-7402 cells as well as cytotoxicity in five cancer cell lines.",

keywords = "Colchicine, HDAC, Hybrid, SAHA, Tubulin",

author = "Xuan Zhang and Jie Zhang and Linjiang Tong and Yu Luo and Mingbo Su and Yi Zang and Jia Li and Wei Lu and Yi Chen",

year = "2013",

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T1 - The discovery of colchicine-SAHA hybrids as a new class of antitumor agents

AU - Zhang, Xuan

AU - Zhang, Jie

AU - Tong, Linjiang

AU - Luo, Yu

AU - Su, Mingbo

AU - Zang, Yi

AU - Li, Jia

AU - Lu, Wei

AU - Chen, Yi

PY - 2013/6/1

Y1 - 2013/6/1

N2 - A novel class of colchicine-SAHA hybrids were designed and synthesised based on the synergistic antitumor effect of tubulin inhibitors and histone deacetylases (HDAC) inhibitors. To the best of our knowledge, this is the first design of molecules that are dual inhibitors of tubulin and HDAC. Biological evaluations of these compounds included the inhibitory activity of HDAC, in vitro cell cycle analysis in BEL-7402 cells as well as cytotoxicity in five cancer cell lines.

AB - A novel class of colchicine-SAHA hybrids were designed and synthesised based on the synergistic antitumor effect of tubulin inhibitors and histone deacetylases (HDAC) inhibitors. To the best of our knowledge, this is the first design of molecules that are dual inhibitors of tubulin and HDAC. Biological evaluations of these compounds included the inhibitory activity of HDAC, in vitro cell cycle analysis in BEL-7402 cells as well as cytotoxicity in five cancer cell lines.

KW - Colchicine

KW - HDAC

KW - Hybrid

KW - SAHA

KW - Tubulin

UR - https://www.scopus.com/pages/publications/84877794404

U2 - 10.1016/j.bmc.2013.03.049

DO - 10.1016/j.bmc.2013.03.049

M3 - 文章

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AN - SCOPUS:84877794404

SN - 0968-0896

VL - 21

SP - 3240

EP - 3244

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 11

ER -

The discovery of colchicine-SAHA hybrids as a new class of antitumor agents

Abstract

UN SDGs

Keywords

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