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

Research output: Contribution to journalArticle

1 Citation (Scopus)

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 languageEnglish (US)
Pages (from-to)239-246
Number of pages8
JournalWuhan University Journal of Natural Sciences
Volume22
Issue number3
DOIs
StatePublished - Jun 1 2017

Fingerprint

Quinazolines
Cytotoxicity
Bioactivity
Antineoplastic Agents
Cells
Phosphorylation
Heterografts
Tumors
Assays
Derivatives
sorafenib

Keywords

  • antitumor agents
  • quinazoline
  • sorafenib analogs
  • synthesis

ASJC Scopus subject areas

  • General

Cite this

Design, synthesis and biological activities of quinazoline containing sorafenib analogs as antitumor agents. / Zhang, Jingwen; Wang, Ningning; Xie, Xiaoxia; Yan, Chunhong; Fu, Fenghua; Yao, Jianwen; Wang, Hongbo.

In: Wuhan University Journal of Natural Sciences, Vol. 22, No. 3, 01.06.2017, p. 239-246.

Research output: Contribution to journalArticle

Zhang, Jingwen ; Wang, Ningning ; Xie, Xiaoxia ; Yan, Chunhong ; Fu, Fenghua ; Yao, Jianwen ; Wang, Hongbo. / Design, synthesis and biological activities of quinazoline containing sorafenib analogs as antitumor agents. In: Wuhan University Journal of Natural Sciences. 2017 ; Vol. 22, No. 3. pp. 239-246.
@article{27e5f3f499a24994bdfbafeec4ada0a9,
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.",
keywords = "antitumor agents, quinazoline, sorafenib analogs, synthesis",
author = "Jingwen Zhang and Ningning Wang and Xiaoxia Xie and Chunhong Yan and Fenghua Fu and Jianwen Yao and Hongbo Wang",
year = "2017",
month = "6",
day = "1",
doi = "10.1007/s11859-017-1241-6",
language = "English (US)",
volume = "22",
pages = "239--246",
journal = "Wuhan University Journal of Natural Sciences",
issn = "1007-1202",
publisher = "Wuhan University",
number = "3",

}

TY - JOUR

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

UR - http://www.scopus.com/inward/record.url?scp=85018779771&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=85018779771&partnerID=8YFLogxK

U2 - 10.1007/s11859-017-1241-6

DO - 10.1007/s11859-017-1241-6

M3 - Article

AN - SCOPUS:85018779771

VL - 22

SP - 239

EP - 246

JO - Wuhan University Journal of Natural Sciences

JF - Wuhan University Journal of Natural Sciences

SN - 1007-1202

IS - 3

ER -