Citation: Xin-Jian Song, Ping Yang, Hui Gao, Yan Wang, Xing-Gao Dong, Xiao-Hong Tan. Facile synthesis and antitumor activity of novel 2-trifl uoromethylthieno[2,3-d]pyrimidine derivatives[J]. Chinese Chemical Letters, ;2014, 25(7): 1006-1010. doi: 10.1016/j.cclet.2014.05.043 shu

Facile synthesis and antitumor activity of novel 2-trifl uoromethylthieno[2,3-d]pyrimidine derivatives

Xin-Jian Song ^a,b,, ,
Ping Yang ^a ,
Hui Gao ^a ,
Yan Wang ^a,, ,
Xing-Gao Dong ^a ,
Xiao-Hong Tan ^a,b

1.
a Key Laboratory of Biologic Resources Protection and Utilization of Hubei Province, Hubei Minzu University, Enshi 445000, China;
2.
b College of Forestry and Horticulture, Hubei Minzu University, Enshi 445000, China

Corresponding author: Xin-Jian Song, Yan Wang,
Received Date: 9 April 2014
Available Online: 21 May 2014
Fund Project: This work was financially supported by the National Natural Science Foundation of China (No. 21262012) (No. 21262012)

A series of novel 2-trifluoromethylthieno[2,3-d]pyrimidine derivatives were synthesized by a facile three-step procedure that afforded advantages of mild reaction conditions, simple protocol and good yields. The structures of the final compounds were confirmed by IR, NMR, EI-MS, elemental analysis, and X-ray diffraction. Preliminary bioassay results showed that some of the analogs exhibit excellent antitumor activity against MCF-7 and HepG2, especially compounds 3a, 3b, 3e and 3h exhibited higher activity than the positive control gefitinib.
- Thieno[2,3-d]pyrimidine,
- Gewald reaction,
- Trifluoromethyl,
- Facile synthesis,
- Antitumor activity
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沈阳化工大学材料科学与工程学院沈阳 110142