Citation: Guo Gang Zhang, Ya Jing Liu, Xiao Guang Ma, Hao Dong, Ju Li, Ping Gong. Synthesis and in vitro cytotoxic evaluation of 2-hydrazinylpyrido[2,3-b]pyrazin-3(4H)-one derivatives[J]. Chinese Chemical Letters, ;2011, 22(10): 1223-1225. doi: 10.1016/j.cclet.2011.05.031 shu

Synthesis and in vitro cytotoxic evaluation of 2-hydrazinylpyrido[2,3-b]pyrazin-3(4H)-one derivatives

Key Laboratory of Original New Drugs Design and Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China

Received Date: 17 March 2011

Fund Project: This work was supported by the grant from National S&T Major Project of China (No.2009ZX09301-012).

A series of novel 2-hydrazinylpyrido[2, 3-b]pyrazin-3 (4H)-one derivatives were synthesized and evaluated for their cytotoxic activities against A549, MDA-MB-231 and HT-29 cell lines in vitro. Pharmacological data indicated that compounds 5b, 5c, 10a and 10g possessed marked cytotoxicity, especially 10a (with IC₅₀ values of 0.81, 2.56 and 1.63 μmol/L against A549, MDA-MB-231 and HT29 cell lines, respectively), which had emerged as a lead compound.
- 2-Hydrazinylpyrido[2,3-b]pyrazin-3(4H)-ones,
- Synthesis,
- Cytotoxicity
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