Synthesis and antiproliferative evaluation of novel tetrahydrobenzo[4 \',5 \']thieno[3 \',2 \':5,6]pyrido[4,3-d] pyrimidine derivativest - 成果

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Synthesis and antiproliferative evaluation of novel tetrahydrobenzo[4 ',5 ']thieno[3 ',2 ':5,6]pyrido[4,3-d] pyrimidine derivativest

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成果类型：

期刊论文

作者：

Tang, Chu;Liang, Yongju;Bai, Shun;He, Hongwu;Chen, Yu;...

通讯作者：

Yang, Guangzhong

作者机构：

[Tang, Chu; Yang, Guangzhong] South Cent Univ Nationalities, Coll Pharm, Lab Nat Prod Chem, Wuhan 430074, Peoples R China.

[Liang, Yongju; Fu, Liwu] Sun Yat Sen Univ, Ctr Canc, State Key Lab Oncol South China, Guangzhou 510060, Guangdong, Peoples R China.

[Bai, Shun; Chen, Yu] South Cent Univ Nationalities, Coll Chem & Mat Sci, Wuhan 430074, Peoples R China.

[He, Hongwu] Cent China Normal Univ, Coll Chem, Wuhan 430079, Peoples R China.

[Yang, Guangzhong] South Cent Univ Nationalities, Coll Pharm, Lab Nat Prod Chem, 128 Minyuan Rd, Wuhan 430074, Peoples R China.

通讯机构：

[Yang, Guangzhong] S

South Cent Univ Nationalities, Coll Pharm, Lab Nat Prod Chem, 128 Minyuan Rd, Wuhan 430074, Peoples R China.

语种：

英文

期刊：

RSC Advances

ISSN：

2046-2069

年：

2014

卷：

期：

页码：

29187-29192

DOI：

10.1039/c4ra03535f

基金类别：

Special Fund for Basic Scientific Research of Central Colleges, South-Central University for Nationalities [CZY13004]

机构署名：

本校为其他机构

院系归属：

化学学院

摘要：

A series of tetrahydrobenzo[4′,5′]thienophene[3′,2′:5,6]pyrido[4,3-d]pyrimidine-4-(3H)-one derivatives were synthesized and evaluated for their antiproliferative activities. Biological evaluation revealed that some compounds exhibited much stronger antiproliferative activity than the positive control Fluorouracil against KB and CEN2 cell lines. Compound 7a exhibited the highest antitumor activity against KB and CNE2 cell lines with IC50 values of 8.18 μM and 13.71 μM, respectively. The preliminary structure-activity relationships showed t...

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Synthesis and antiproliferative evaluation of novel tetrahydrobenzo[4 ',5 ']thieno[3 ',2 ':5,6]pyrido[4,3-d] pyrimidine derivativest

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