Citation: Qin Ming-Ze, Wang Lei, Yan Shuang, Ma Jun-Jie, Tian Ye, Zhao Yan-Fang, Gong Ping. Identification of hydrazone moiety-bearing aminopyrimidines as potent antitumor agents with selective inhibition of gefitinib-resistant H1975 cancer cells[J]. Chinese Chemical Letters, ;2017, 28(5): 991-994. doi: 10.1016/j.cclet.2016.11.030 shu

Identification of hydrazone moiety-bearing aminopyrimidines as potent antitumor agents with selective inhibition of gefitinib-resistant H1975 cancer cells

Qin Ming-Ze ^a,, ,
Wang Lei ^a ,
Yan Shuang ^a ,
Ma Jun-Jie ^b ,
Tian Ye ^a ,
Zhao Yan-Fang ^a ,
Gong Ping ^a,,

a.
Key Laboratory of Structure-Based Drug Design and Discovery(Shenyang Pharmaceutical University), Ministry of Education, Shenyang 110016, China
b.
School of Biomedical Sciences, Huaqiao University, Quanzhou 362021, China

Corresponding author: Qin Ming-Ze, qinmingze001@126.com Gong Ping, gongpinggp@126.com
Received Date: 5 September 2016
Revised Date: 30 October 2016
Accepted Date: 11 November 2016
Available Online: 27 May 2016

Figures(3)

Based on our previous work, a series of hydrazone moiety-bearing aminopyrimidines were synthesized. The compounds were evaluated for inhibitory activities against EGFR T790M/L858R and antiproliferative activities against H1975 and A549 NSCLC cell lines harboring different forms of EGFR. Compounds 7f and 7k exhibited potent and selective activity in inhibition of gefitinib-resistant H1975 cancer cells (IC₅₀; 0.45, 0.2 μmol/L) while were much less active on A549 cancer cells (IC₅₀; 52.83, > 100 μmol/L). Both compounds could be served as promising lead compounds for further investigation.
- Aminopyrimidines,
- EGFR T790M/L858R,
- Selectivity,
- Anti-resistance,
- Antiproliferative activity
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沈阳化工大学材料科学与工程学院沈阳 110142