Key Laboratory of Original New Drugs Design and Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang, P. R. China.
Arch Pharm (Weinheim). 2012 Jan;345(1):49-56. doi: 10.1002/ardp.201100103. Epub 2011 Sep 23.
In an attempt to develop potent antitumor agents, a series of novel 2-hydrazonylpyrido[2,3-b]pyrazin-3(4H)-one derivatives were designed and synthesized. All the prepared compounds were screened for their cytotoxic activities against A549, MDA-MB-231 and HT-29 cell lines in vitro. Pharmacological data indicated that five of the target compounds showed cytotoxicity against A549 cell line below a concentration of 1 µM. Compound 15g was the most potent one with IC(50) values of 0.19, 2.11 and 2.15 µM against A549, MDA-MB-231 and HT29 cell lines, respectively.
为了开发有效的抗肿瘤药物，设计并合成了一系列新型 2-酰腙基吡啶并[2,3-b]吡嗪-3(4H)-酮衍生物。所有制备的化合物均进行了体外细胞毒性活性筛选，以评估其对 A549、MDA-MB-231 和 HT-29 细胞系的抑制活性。药理数据表明，有 5 种目标化合物对 A549 细胞系的抑制活性低于 1μM。化合物 15g 的抑制活性最强，对 A549、MDA-MB-231 和 HT-29 细胞系的 IC50 值分别为 0.19、2.11 和 2.15μM。
