TY - JOUR
T1 - Synthesis and antitumor activity of α-aminophosphonate derivatives containing thieno[2,3-d]pyrimidines
AU - Guo, Yan Chun
AU - Li, Jing
AU - Ma, Jiao Li
AU - Yu, Zhi Ran
AU - Wang, Hai Wei
AU - Zhu, Wen Juan
AU - Liao, Xin Cheng
AU - Zhao, Yu Fen
N1 - Funding Information:
This work was supported by the National Natural Sciences Foundations of China (Nos. 21171149, 21105091 ). We are grateful to Pro. Yanbing Zhang’ group for performing in vitro antitumor activity evaluation.
PY - 2015
Y1 - 2015
N2 - Abstract Two series of thieno[2,3-d]pyrimidine derivatives were designed and synthesized, in which bioactive α-aminophosphonate subunits were introduced at the N3 position through an NN bond connection. The in vitro cytotoxic activity of the novel compounds was tested against human esophageal carcinoma cells (EC109), human hepatocarcinoma cells (HepG2), human gastric carcinoma cells (MGC-803), respectively, by the MTT method. The evaluation results revealed that compounds 6mb, 6mf, 6mg, 6nd and 6nh exerted the most potent inhibition against HepG2, MGC-803 and EC109 cells, respectively. In particular, compound 6mg presented excellent inhibitory effect against HepG2 (91.2%) and MGC-803 (94.4%) cells.
AB - Abstract Two series of thieno[2,3-d]pyrimidine derivatives were designed and synthesized, in which bioactive α-aminophosphonate subunits were introduced at the N3 position through an NN bond connection. The in vitro cytotoxic activity of the novel compounds was tested against human esophageal carcinoma cells (EC109), human hepatocarcinoma cells (HepG2), human gastric carcinoma cells (MGC-803), respectively, by the MTT method. The evaluation results revealed that compounds 6mb, 6mf, 6mg, 6nd and 6nh exerted the most potent inhibition against HepG2, MGC-803 and EC109 cells, respectively. In particular, compound 6mg presented excellent inhibitory effect against HepG2 (91.2%) and MGC-803 (94.4%) cells.
KW - Antitumor
KW - Synthesis
KW - Thieno[2,3-d]pyrimidine
KW - α-Aminophosphonate derivatives
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U2 - 10.1016/j.cclet.2015.03.026
DO - 10.1016/j.cclet.2015.03.026
M3 - Article
AN - SCOPUS:84937390024
VL - 26
SP - 755
EP - 758
JO - Chinese Chemical Letters
JF - Chinese Chemical Letters
SN - 1001-8417
IS - 6
M1 - 3255
ER -