Citation: Wang Shenghong, Han Xiao, Mao Ting, Zeng Huijun, Chen Rui, Chen Huiqiong. Synthesis and Antitumor Activity Evaluation of Novel Tetrahydrobenzo[4', 5']thieno[3', 2': 5, 6]pyrido[4, 3-d]pyrimidine Derivatives[J]. Chemistry, ;2019, 82(7): 623-629. shu

Synthesis and Antitumor Activity Evaluation of Novel Tetrahydrobenzo[4', 5']thieno[3', 2': 5, 6]pyrido[4, 3-d]pyrimidine Derivatives

1.
Changjiang Polytechnic, Wuhan 430064
2.
Wuhan Institute for Food and Cosmetic Control, Wuhan 430012
3.
Wuhan Institute of Technology, Wuhan 430205
4.
Wuhan Aimin Pharmaceutical Limited company, Ezhou 436070

Corresponding author: Han Xiao, hxiao12378@126.com
Received Date: 24 February 2019
Accepted Date: 16 March 2019

Figures(1)

A series of novel tetrahydrobenzo[4', 5']thieno[3', 2':5, 6]pyrido[4, 3-d]pyrimidine derivatives were designed and synthesized via a tandem aza-Wittig reaction, and their anti-tumor activities in vitro were evaluated for CNE2, KB, MGC-803, MCF-7 and PC3 cells by MTT assay. The preliminary biological results showed that these conjugates display significant antiproliferative effect on these five cancer cells, especially for MGC-803. Compound 8c (IC₅₀=0.9±0.25μmol·L^-1) stood out as the most potent compound against MGC-803, and is 20 times more active than 5-FU (IC₅₀=18.4±1.43μmol·L^-1). Additionally, all compounds were nontoxic to health GES-1 and VERO cells, while 5-FU showed essential toxicity. Tetrahydrobenzo[4', 5'] thieno[3', 2':5, 6] pyrido[4, 3-d] pyrimidine compounds displayed good anti-tumor activity and deserved further research.
- Aza-Wittig reaction,
- Tetrahydrobenzo[4', 5']thieno,
- [3', 2':5, 6]Pyrido[4, 3-d]pyrimidine,
- Antitumor
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沈阳化工大学材料科学与工程学院沈阳 110142