Synthesis and Antitumor Activity of Novel Terephthalamide Derivatives

被引：0

作者：

Gu, Yifei ^{[1
,2
]}

Wu, Caiju ^{[1
]}

Wang, Siqi ^{[1
]}

Zhang, Shilin ^{[1
]}

Lu, Yuan ^{[1
]}

Si, Xinxin ^{[1
]}

Jiang, Bailing ^{[3
]}

机构：

[1] Jiangsu Ocean Univ, Coll Pharm, Jiangsu Key Laborratory Marine Pharmaceut Cpd Scre, Lianyungang 222005, Jiangsu, Peoples R China

[2] Jiangsu Inst Marine Resources Dev, Lianyungang 222005, Jiangsu, Peoples R China

[3] Second Peoples Hosp Lianyungang, Dept Pharm, Lianyungang 222005, Jiangsu, Peoples R China

来源：

CHINESE JOURNAL OF ORGANIC CHEMISTRY | 2024年 / 44卷 / 11期

关键词：

terephthalamide; antivity; synthesis;

D O I：

10.6023/cjoc202403049

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

In order to search for new structural antitumor drugs, a series of terephthalamide derivatives were designed and synthesized, and their antiproliferative activities against human tumor cell lines (PANC-1, MDA-MB-231 and SGC7901) were determined. N-1-(4-Methoxybenzyl)-N-4-(3-methoxyphenyl)-N-1-(3,4,5-trimethoxyphenyl)terephthalamide (TF) was identified as the most potent compound in antiproliferation against PANC-1 cells with the value of 0.13 mu mol/L, which was better than the positive control 5-fluorouracil (16.22 mu mol/L). Further mechanistic studies showed that compound TF could inhibit the clonal proliferation in a dose-dependent manner. In addition, compound TF can reduce the adhesive, migrational and invasive of PANC-1cells. These results indicated that compound TF might be developed the antitumor drug.

引用

页码：3497 / 3504

页数：8