Synthesis and antiproliferative evaluation of new hybrids of piperine and acylhydrazone

被引：0

作者：

Xu, Shi-Kun ^{[1
]}

Jia, Zi-Ming ^{[2
]}

Liu, Wen-Qi ^{[3
]}

Gu, Yin-Zi ^{[3
]}

Xi, Jia-He ^{[3
]}

Xu, Jing ^{[3
]}

Yang, Guang-Zhong ^{[3
]}

Yang, Xin-Zhou ^{[3
]}

Chen, Yu ^{[1
]}

机构：

[1] South Cent Minzu Univ, Coll Chem & Mat Sci, Wuhan, Peoples R China

[2] Hubei Prov Ctr Dis Control & Prevent, Wuhan, Peoples R China

[3] South Cent Minzu Univ, Sch Pharmaceut Sci, Ethnopharmacol Level Lab 3, Wuhan, Peoples R China

来源：

NATURAL PRODUCT RESEARCH | 2024年

关键词：

Piperine; piperine-base acylhydrazone derivatives; antiproliferative evaluation; NATURAL-PRODUCTS; DESIGN;

D O I：

10.1080/14786419.2024.2391083

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

Piperine, a natural amide isolated from the genus of Piper, serves as a pharmacophore in medicinal chemistry. In this study, we synthesised and evaluated 18 novel piperine-acylhydrazone hybrids (4a-4r) for their antiproliferative activities in vitro. The structures of these hybrids were validated using H-1,C-13 NMR, and HR-ESI-MS data. Furthermore, we screened all synthesised compounds for their antiproliferative activities against three human cancer cell lines: FaDu (laryngeal carcinoma cells), HepG2 (hepatoblastoma carcinoma cells), and MGC803 (gastric carcinoma cells). Among them, compound 4o exhibited significantly inhibitory activities against FaDu, HepG2, and MGC803 with IC50 values of 13.85 +/- 0.19, 11.02 +/- 1.45, and 13.47 +/- 3.43 mu M, respectively, which was approximately two-fold lower than the positive control cisplatin. These findings suggest that compound 4o has the potential to be promising leads for the design of anti-cancer drugs.

引用

页数：6