Design, synthesis and biological activities of quinazoline containing sorafenib analogs as antitumor agents

Jingwen Zhang; Ningning Wang; Xiaoxia Xie; Chunhong Yan; Fenghua Fu; Jianwen Yao; Hongbo Wang

doi:10.1007/s11859-017-1241-6

Design, synthesis and biological activities of quinazoline containing sorafenib analogs as antitumor agents

Jingwen Zhang, Ningning Wang, Xiaoxia Xie, Chunhong Yan, Fenghua Fu, Jianwen Yao, Hongbo Wang

Biochemistry and Molecular Biology

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

2 Scopus citations

Abstract

A series of novel sorafenib derivatives containing quinazoline moiety were designed and synthesized. Their antiproliferative activities against HCT116 and HCT115 cell lines were evaluated using MTT assay. Most of the synthesized compounds showed significant cytotoxicity against the selected cell lines. These cytotoxicities were consistent with their inhibitory activity against the phosphorylation of c-Raf, MEK1/2 and ERK1/2. Compound GD-09 also showed much stronger anti-tumor activity than that of sorafenib in vivo by B16 melanoma xenograft model test.

Original language	English (US)
Pages (from-to)	239-246
Number of pages	8
Journal	Wuhan University Journal of Natural Sciences
Volume	22
Issue number	3
DOIs	https://doi.org/10.1007/s11859-017-1241-6
State	Published - Jun 1 2017

Keywords

antitumor agents
quinazoline
sorafenib analogs
synthesis

ASJC Scopus subject areas

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10.1007/s11859-017-1241-6

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title = "Design, synthesis and biological activities of quinazoline containing sorafenib analogs as antitumor agents",

abstract = "A series of novel sorafenib derivatives containing quinazoline moiety were designed and synthesized. Their antiproliferative activities against HCT116 and HCT115 cell lines were evaluated using MTT assay. Most of the synthesized compounds showed significant cytotoxicity against the selected cell lines. These cytotoxicities were consistent with their inhibitory activity against the phosphorylation of c-Raf, MEK1/2 and ERK1/2. Compound GD-09 also showed much stronger anti-tumor activity than that of sorafenib in vivo by B16 melanoma xenograft model test.",

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author = "Jingwen Zhang and Ningning Wang and Xiaoxia Xie and Chunhong Yan and Fenghua Fu and Jianwen Yao and Hongbo Wang",

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T1 - Design, synthesis and biological activities of quinazoline containing sorafenib analogs as antitumor agents

AU - Zhang, Jingwen

AU - Wang, Ningning

AU - Xie, Xiaoxia

AU - Yan, Chunhong

AU - Fu, Fenghua

AU - Yao, Jianwen

AU - Wang, Hongbo

PY - 2017/6/1

Y1 - 2017/6/1

N2 - A series of novel sorafenib derivatives containing quinazoline moiety were designed and synthesized. Their antiproliferative activities against HCT116 and HCT115 cell lines were evaluated using MTT assay. Most of the synthesized compounds showed significant cytotoxicity against the selected cell lines. These cytotoxicities were consistent with their inhibitory activity against the phosphorylation of c-Raf, MEK1/2 and ERK1/2. Compound GD-09 also showed much stronger anti-tumor activity than that of sorafenib in vivo by B16 melanoma xenograft model test.

AB - A series of novel sorafenib derivatives containing quinazoline moiety were designed and synthesized. Their antiproliferative activities against HCT116 and HCT115 cell lines were evaluated using MTT assay. Most of the synthesized compounds showed significant cytotoxicity against the selected cell lines. These cytotoxicities were consistent with their inhibitory activity against the phosphorylation of c-Raf, MEK1/2 and ERK1/2. Compound GD-09 also showed much stronger anti-tumor activity than that of sorafenib in vivo by B16 melanoma xenograft model test.

KW - antitumor agents

KW - quinazoline

KW - sorafenib analogs

KW - synthesis

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SN - 1007-1202

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JO - Wuhan University Journal of Natural Sciences

JF - Wuhan University Journal of Natural Sciences

IS - 3

ER -

Design, synthesis and biological activities of quinazoline containing sorafenib analogs as antitumor agents

Abstract

Keywords

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