Synthesis and Antitumor Activity of 2,4,6-Trisubstituted Novel Quinazoline Derivatives Containing Trifluoromethyl

被引：0

作者：

Wang Zhengjie ^{[1
,2
]}

Dai Honglin ^{[1
,2
]}

Si Xiaojie ^{[1
,2
]}

Gao Chao ^{[1
,2
]}

Liu Limin ^{[1
,2
]}

Zhang Luye ^{[1
,2
]}

Zhang Yang ^{[1
,2
]}

Song Yadan ^{[1
,2
]}

Zhao Peirong ^{[1
,2
,3
]}

Zheng Jiaxin ^{[1
,2
]}

Ke Yu ^{[1
,2
]}

Liu Hongmin ^{[1
,2
,3
,4
]}

Zhang Qiurong ^{[1
,2
,4
]}

机构：

[1] Zhengzhou Univ, Sch Pharmaceut Sci, Zhengzhou 450001, Peoples R China

[2] Zhengzhou Univ, Collaborat Innovat Ctr New Drug Res & Safety Eval, Zhengzhou 450001, Peoples R China

[3] Zhengzhou Univ, State Key Lab Esophageal Canc Prevent & Treatment, Zhengzhou 450052, Peoples R China

[4] Zhengzhou Univ, Minist Educ China, Key Lab Adv Drug Preparat Technol, Zhengzhou 450001, Peoples R China

来源：

CHINESE JOURNAL OF ORGANIC CHEMISTRY | 2022年 / 42卷 / 01期

基金：

中国国家自然科学基金;

关键词：

trifluoromethyl; quinazoline; synthesis; antitumor activity; INHIBITORS; DESIGN; SAR;

D O I：

10.6023/cjoc202107026

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

In order to find efficient and low toxicity antitumor drugs, a series of novel 2,4,6-trisubstituted quinazoline derivatives containing trifluoromethyl were synthesized and evaluated for their antitumor activities against human cancer cell lines (PC-3, MCF-7, Eca-109, MGC-803, HGC-27, A549, H1975) by using methyl thiazolyl tetrazolium (MTT) assay. Most of compounds exerted moderate to excellent antitumor activity against seven human cancer cells. Among them, N-(3-bromophenyl)-6-methoxy-2-04-(trifluoromethyl)benzyl)thio)quinazolin-4-amine (161) showed the best antitumor activity against PC-3 cancer cell line, with the IC50 values of (2.22 +/- 0.15) mu mol/L, which was better than the positive control of gefitinib. At the same time, and compound 161 could dose-dependently and time-dependently induce PC-3 cells apoptosis.

引用

页码：249 / 256

页数：8

共 27 条

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