Citation: Lin Li, Cun-Long Zhang, Hong-Rui Song, Chun-Yan Tan, Huai-Wei Ding, Yu-Yang Jiang. Discovery of novel dual inhibitors of VEGFR and PI3K kinases containing 2-ureidothiazole scaffold[J]. Chinese Chemical Letters, ;2016, 27(01): 1-6. doi: 10.1016/j.cclet.2015.09.008 shu

Discovery of novel dual inhibitors of VEGFR and PI3K kinases containing 2-ureidothiazole scaffold

Lin Li ^a,c ,
Cun-Long Zhang ^a,c ,
Hong-Rui Song ^b ,
Chun-Yan Tan ^a,c ,
Huai-Wei Ding ^a,b,, ,
Yu-Yang Jiang ^a,c,,

1.
a Department of Chemistry, Tsinghua University, Beijing 100084, China;
2.
b School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110000, China;
3.
c The Graduate School at Shenzhen, Tsinghua University, Shenzhen 518000, China

Corresponding author: Huai-Wei Ding, Yu-Yang Jiang,
Received Date: 22 April 2015
Available Online: 15 May 2015
Fund Project: The authors would like to thank the financial supports from the NSFC(No. 21272134) (No. 21272134)Shenzhen Municipal government SZSITIC(Nos. JCYJ20130402145002384, ZDSY20120619141412872). (Nos. JCYJ20130402145002384, ZDSY20120619141412872)

A series of compounds possessing 2-(3-phenyl)ureidothiazol-4-formamide derivatives with a 2-ureidothiazole scaffold were designed and synthesized. Some compounds demonstrated inhibition of cell proliferation against both MDA-MB-231 and HepG2 cell lines using Sorafenib as the positive control. Compounds 6i showed a good to moderate inhibition on VEGFR-2 and PI3Kα which was proved by further molecular docking study. This study suggests that compound 6i is a potential dual inhibitor of VEGFR-2 and PI3Kα and is applicable for further investigation.
- 2-Aminothiazole,
- VEGFR,
- PI3K,
- Anticancer
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