Synthesis and Antitumor Activity of Some Novel 5,6,7,8-Tetrahydrobenzo-thieno[2,3-d]pyrimidin-4(3H)-one Derivatives

被引：11

作者：

Wang, Hongmei ^{[1
,2
]}

Guo, Shubing ^{[3
]}

Hu, Yanggen ^{[1
,2
,4
]}

Zeng, Xiaohua ^{[1
,2
]}

Yang, Guangyi ^{[1
,2
,4
]}

机构：

[1] Hubei Univ Med, Hubei Key Lab Wudang Local Chinese Med Res, Shiyan 442000, Peoples R China

[2] Hubei Univ Med, Inst Med Chem, Shiyan 442000, Peoples R China

[3] Lib Hubei Univ Med, Shiyan 442000, Peoples R China

[4] Hubei Univ Med, Taihe Hosp, Dept Pharm, Shiyan 442000, Peoples R China

来源：

CHINESE JOURNAL OF ORGANIC CHEMISTRY | 2015年 / 35卷 / 05期

关键词：

aza-Wittig reaction; thieno[2,3-d]pyrimidin-4(3H)-ones; synthesis; antitumor; BIOLOGICAL EVALUATION; EFFICIENT SYNTHESIS; DESIGN;

D O I：

10.6023/cjoc201410035

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The aza-Wittig reaction of iminophosphorane 2 with alkyl isocyanates gave carbodiimides 3, which were allowed to react with various nucleophilic reagents under mild condition in satisfactory yields to prepare a novel series of 5,6,7,8-tetrahydrobenzothieno[2,3-d]pyrimidin-4(3H)-one derivatives. The structures of these compounds were confirmed by H-1 NMR, IR, MS and elemental analysis. The in vitro antitumor activities of compounds were analyzed with 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazo-liumbromide (MTT) standard method, 5d stood out as the most potent showing an IC50 of 19.0 mu mol/L against human tumor cell lines (KB).

引用

页码：1075 / 1080

页数：6

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