Synthesis and Antitumor Activities of Novel 1,2,3-Triazolo[4,5-<i>d</i>]pyrimidine Derivatives

栗娜,; 辛景超,; 马启胜,; 李二冬,; 孟娅琪,; 包崇男,; 杨鹏,; 宋攀攀,; 崔飞,; 陈鹏举,; 顾一飞,; 赵培荣,; 可钰,; 刘宏民,; 张秋荣,

doi:10.6023/cjoc201709030

Cited by 4 publications

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“…[1] Statistics show that approximately 13.15 million people will die from cancer until 2035. [2] Chemotherapy is a very important method in clinic. However, Many anti-tumor drugs are prone to drug resistance.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Antitumor Activity of Novel Quinazoline Derivatives Containing Acrylamide

Zhang¹,

Zhang²,

Wang³

et al. 2020

Chin. J. Org. Chem.

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In order to find efficient and low toxicity anti-tumor drugs, a series of novel quinazoline derivatives containing N-(3-aminophenyl)acrylamide were synthesized and their antiproliferative activities were evaluated against three human cancer cell lines (H1975, PC-3, MGC-803) by using methyl thiazolyl tetrazolium (MTT) assay. The results showed that most compounds exhibited better antiproliferative activities against the four human tumor cell lines. Among them, N-(3-(2-((4-((4-chlorophenyl)amino)-7-methoxy-quinazolin-6-yl)oxy)acetamido)phenyl)acrylamide (13j) showed the best antiproliferative activity against H1975 and MGC-803 cancer cell lines with IC 50 values of (6.77±0.65) and (4.06±0.34) μmol/L, respectively. Its activity was better than the positive control gefitinib. In a nutshell, this work provides clues to discover antitumor agent based on the quinazoline scaffold.

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Section: Introductionmentioning

confidence: 99%