Design, synthesis and biological evaluation of C(6)-modified celastrol derivatives as potential antitumor agents

Kaiyong Tang; Qingqing Huang; Jafeng Zeng; Guangming Wu; Jinwen Huang; Junfang Pan; Wei Lu

doi:10.3390/molecules190710177

Design, synthesis and biological evaluation of C(6)-modified celastrol derivatives as potential antitumor agents

Kaiyong Tang
, Qingqing Huang
, Jafeng Zeng
, Guangming Wu
, Jinwen Huang
, Junfang Pan^*
, Wei Lu

^*Corresponding author for this work

School of Chemistry and Molecular Engineering

East China Normal University
Shanghai Hotmed Sciences Co., Ltd.

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

39 Scopus citations

Abstract

New six C6-celastrol derivatives were designed, synthesized, and evaluated for their in vitro cytotoxic activities against nine human cancer cell lines (BGC-823, H4, Bel7402, H522, Colo 205, HepG2 and MDA-MB-468). The results showed that most of the compounds displayed potent inhibition against BGC823, H4, and Bel7402, with IC50s of 1.84-0.39 μM. The best compound NST001A was tested in an in vivo antitumor assay on nude mice bearing Colo 205 xenografts, and showed significant inhibition of tumor growth at low concentrations. Therefore, celastrol C-6 derivatives are potential drug candidates for treating cancer.

Original language	English
Pages (from-to)	10177-10188
Number of pages	12
Journal	Molecules
Volume	19
Issue number	7
DOIs	https://doi.org/10.3390/molecules190710177
State	Published - Jul 2014

UN SDGs

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

SDG 3 Good Health and Well-being

Keywords

Antitumor activity
Celastrol C-6 derivatives
In vitro
In vivo

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10.3390/molecules190710177

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title = "Design, synthesis and biological evaluation of C(6)-modified celastrol derivatives as potential antitumor agents",

abstract = "New six C6-celastrol derivatives were designed, synthesized, and evaluated for their in vitro cytotoxic activities against nine human cancer cell lines (BGC-823, H4, Bel7402, H522, Colo 205, HepG2 and MDA-MB-468). The results showed that most of the compounds displayed potent inhibition against BGC823, H4, and Bel7402, with IC50s of 1.84-0.39 μM. The best compound NST001A was tested in an in vivo antitumor assay on nude mice bearing Colo 205 xenografts, and showed significant inhibition of tumor growth at low concentrations. Therefore, celastrol C-6 derivatives are potential drug candidates for treating cancer.",

keywords = "Antitumor activity, Celastrol C-6 derivatives, In vitro, In vivo",

author = "Kaiyong Tang and Qingqing Huang and Jafeng Zeng and Guangming Wu and Jinwen Huang and Junfang Pan and Wei Lu",

year = "2014",

month = jul,

doi = "10.3390/molecules190710177",

language = "英语",

volume = "19",

pages = "10177--10188",

journal = "Molecules",

issn = "1420-3049",

publisher = "Multidisciplinary Digital Publishing Institute (MDPI)",

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}

TY - JOUR

T1 - Design, synthesis and biological evaluation of C(6)-modified celastrol derivatives as potential antitumor agents

AU - Tang, Kaiyong

AU - Huang, Qingqing

AU - Zeng, Jafeng

AU - Wu, Guangming

AU - Huang, Jinwen

AU - Pan, Junfang

AU - Lu, Wei

PY - 2014/7

Y1 - 2014/7

N2 - New six C6-celastrol derivatives were designed, synthesized, and evaluated for their in vitro cytotoxic activities against nine human cancer cell lines (BGC-823, H4, Bel7402, H522, Colo 205, HepG2 and MDA-MB-468). The results showed that most of the compounds displayed potent inhibition against BGC823, H4, and Bel7402, with IC50s of 1.84-0.39 μM. The best compound NST001A was tested in an in vivo antitumor assay on nude mice bearing Colo 205 xenografts, and showed significant inhibition of tumor growth at low concentrations. Therefore, celastrol C-6 derivatives are potential drug candidates for treating cancer.

AB - New six C6-celastrol derivatives were designed, synthesized, and evaluated for their in vitro cytotoxic activities against nine human cancer cell lines (BGC-823, H4, Bel7402, H522, Colo 205, HepG2 and MDA-MB-468). The results showed that most of the compounds displayed potent inhibition against BGC823, H4, and Bel7402, with IC50s of 1.84-0.39 μM. The best compound NST001A was tested in an in vivo antitumor assay on nude mice bearing Colo 205 xenografts, and showed significant inhibition of tumor growth at low concentrations. Therefore, celastrol C-6 derivatives are potential drug candidates for treating cancer.

KW - Antitumor activity

KW - Celastrol C-6 derivatives

KW - In vitro

KW - In vivo

UR - https://www.scopus.com/pages/publications/84904808084

U2 - 10.3390/molecules190710177

DO - 10.3390/molecules190710177

M3 - 文章

C2 - 25025148

AN - SCOPUS:84904808084

SN - 1420-3049

VL - 19

SP - 10177

EP - 10188

JO - Molecules

JF - Molecules

IS - 7

ER -

Design, synthesis and biological evaluation of C(6)-modified celastrol derivatives as potential antitumor agents

Abstract

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Keywords

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