Synthesis and Antitumor Activity of Novel N-Benzoyl-N′-substituted Pyrimidinyl (Thio)semicarbazide Derivatives

被引：2

作者：

Song, Gaopeng ^{[1
]}

Li, Jianzuo ^{[2
]}

Tian, Hao ^{[1
]}

Li, Yasheng ^{[1
]}

Hu, Dekun ^{[1
]}

Li, Ying ^{[2
]}

Cui, Zining ^{[1
]}

机构：

[1] South China Agr Univ, Guangdong Prov Key Lab Microbial Signals & Dis Co, Guangzhou 510642, Guangdong, Peoples R China

[2] Shandong Agr Univ, Coll Chem & Mat Sci, Tai An 271018, Shandong, Peoples R China

来源：

LETTERS IN DRUG DESIGN & DISCOVERY | 2016年 / 13卷 / 04期

基金：

中国国家自然科学基金;

关键词：

Synthesis; (thio)semicarbazide; antitumor activity; multidrug resistance; EFFECTIVE ANTIPROLIFERATIVE AGENTS; PYRIDOXAL ISONICOTINOYL HYDRAZONE; IRON CHELATORS; RIBONUCLEOTIDE REDUCTASE; CELL-GROWTH; BIOACTIVITY; POTENT; INHIBITION; SALICYLALDEHYDE; NEUROBLASTOMA;

D O I：

10.2174/1570180812666151003002644

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of substituted pyrimidinyl (thio) semicarbazide derivatives were designed and synthesized. The antitumor results showed that the activity of thiosemicarbazide compounds (series II) was generally higher than that of the corresponding semicarbazide derivatives (series I). Among them, IIk displayed higher cytotoxicity against HL-60, BGC-823 and Bel-7402 than that of adriamycin and exhibited broad in vitro cytotoxicity against 13 human tumor cell lines. Meanwhile, the cytotoxic selectivity and anti-multidrug resistance were evaluated, and IIk exhibited selective cytotoxicity against cancer cells in comparison to human normal cells and had significant anti-multidrug resistance capability. The bioassay results showed that IIk showed great promise as a potent lead compound for further antitumor discovery.

引用

页码：329 / 334

页数：6

共 31 条

[1] EVALUATION OF THE IRON CHELATION POTENTIAL OF HYDRAZONES OF PYRIDOXAL, SALICYLALDEHYDE AND 2-HYDROXY-1-NAPHTHYLALDEHYDE USING THE HEPATOCYTE IN CULTURE [J].