Here, two series of 17-hydrazone derivatives and D-fused pyrazoline derivatives possessing various aromatic heterocycle structures from androstenedione were synthesized and their structures were evaluated. The antiproliferative activity of synthesized compounds against three cancer cells (446, Eca-109, AGS) and a normal cell line (GES-1) was investigated. Cisplatin was taken as the reference drug. The results have demonstrated that D-fused pyrazoline derivatives showed strong activity than 17-hydrazone derivatives. Compound 7b, bearing a phenyl group at 5 in pyrazoline, inhibits the growth of Eca-109, 446 and AGS cells with IC50=17.5, 25.3, 27.4M, respectively. The corresponding IC50 of cisplatin is 30.4, 44.2, 36.7M. This suggests it is a potent apoptotic inducer in these carcinoma cells. Most of the compounds show very weak toxicity towards GES-1 normal cell line.
基金：
National Natural Science Foundation of P. R. ChinaNational Natural Science Foundation of China (NSFC) [81772550, 81502032, 21603053]; Program of Science and Technology of Hebei [17211412]; Project of Hebei University of Science and Technology [1182120]
第一作者机构：[1]Hebei Univ Sci & Technol, Coll Sci, Shijiazhuang 050018, Hebei, Peoples R China
通讯作者：
通讯机构：[2]Hebei Med Univ, Hosp 4, Res Ctr, Shijiazhuang 050011, Hebei, Peoples R China
推荐引用方式(GB/T 7714)：
Chen Shaorui,Wu Hao,Li Ai-jun,et al.Synthesis and biological evaluation of hydrazone and pyrazoline derivatives derived from androstenedione[J].RESEARCH ON CHEMICAL INTERMEDIATES.2018,44(11):7029-7046.doi:10.1007/s11164-018-3539-1.
APA：
Chen, Shaorui,Wu, Hao,Li, Ai-jun,Pei, Juan&Zhao, Lianmei.(2018).Synthesis and biological evaluation of hydrazone and pyrazoline derivatives derived from androstenedione.RESEARCH ON CHEMICAL INTERMEDIATES,44,(11)
MLA：
Chen, Shaorui,et al."Synthesis and biological evaluation of hydrazone and pyrazoline derivatives derived from androstenedione".RESEARCH ON CHEMICAL INTERMEDIATES 44..11(2018):7029-7046
