Chinese Journal of Organic Chemistry >
Synthesis and Antitumor Activity of Amide Derivatives Containing 1,3,4-Thiadiazole and Pyrazole Moieties
Received date: 2021-02-18
Revised date: 2021-03-30
Online published: 2021-05-14
Supported by
National Natural Science Foundation of China(22078072); Guangdong Basic and Applied Basic Research Foundation(2019A1515110346); Science and Technology Plan of Maoming(2019401); Science and Technology Plan of Maoming(2020581); Doctor Startup Project of Guangdong University of Petrochemical Technology(517152); Doctor Startup Project of Guangdong University of Petrochemical Technology(2019rc053); Young Creative Talents Training Project of Guangdong University of Petrochemical Technology(517136)
In this work, a series of newly-synthesized amide derivatives (A1~A26) carrying 1,3,4-thiadiazole and pyrazole moieties were successfully designed and synthesized. In addition, their structures were characterized by multiple techniques including 1H NMR, 13C NMR, IR, ESI-MS and HRMS. Furthermore, based on the antitumor results against human hepatocarcinoma cells (HepG2) and human gastric carcinoma cells (MGC803) via methyl thiazolyl tetrazolium (MTT) method, the in vitro cytotoxic activities of the compounds were evaluated, indicating that compounds A1 (IC50=0.0695 μmol/mL), A2 (IC50=0.0682 μmol/mL) and A3 (IC50=0.0753 μmol/mL) exhibited similar inhibitory effect against HepG2 cells. More importantly, compound A1 displayed superior inhibition performance against MGC803 cells (IC50=0.0420 μmol/mL) compared with that of 5-fluorouracil (IC50=0.0820 μmol/mL).
Jiaoli Ma , Penghu Guo , Jing Li , Xincheng Liao , Huicheng Cheng . Synthesis and Antitumor Activity of Amide Derivatives Containing 1,3,4-Thiadiazole and Pyrazole Moieties[J]. Chinese Journal of Organic Chemistry, 2021 , 41(8) : 3214 -3222 . DOI: 10.6023/cjoc202102030
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