Letters in Drug Design & Discovery ( IF 1.2 ) Pub Date : 2015-01-31 , DOI: 10.2174/1570180811666140909010017 Lei Zhang , Jing Wang , Wen-Yun Li , Juan Xia , Jing Gao , Qi-Zheng Yao
A series of hybrids of 3-hydroxy-indolin-2-one and 2,3-dihydroquinolin-4(1H) -one were synthesized and their anti-proliferative activities against two human cancer cell lines were initially evaluated. Compound 7g was selected for further study and demonstrated moderate anti-proliferative activities against four human cancer cell lines. Meanwhile, 7g had inhibitory effects on the growth of SGC-7901 cells in dosage-and time-dependent manners and the cancer cells appeared morphological changes. Moreover, 7g was more effective in the inhibition of xenografted tumor in vivo growth and mice treated with 7g showed more weight gain than 5-FU-treated mice over the treatment period, suggesting a lower toxic effect than 5-FU. After treatment with 7g, the tumor showed typical morphological changes as evaluated by H&E staining.
中文翻译:
3-羟基吲哚-2-酮和2,3-二氢喹啉-4(1H)-一的杂合物的合成,体外和体内抗癌活性
合成了一系列3-羟基-吲哚-2--2-和2,3-二氢喹啉-4(1H)-的杂合体,并初步评估了它们对两种人类癌细胞系的抗增殖活性。选择化合物7g进行进一步研究,并证明其对四种人类癌细胞系具有中等程度的抗增殖活性。同时,7g对SGC-7901细胞的生长具有剂量和时间依赖性的抑制作用,癌细胞出现形态学改变。此外,在整个治疗期间,7g抑制异种移植肿瘤的体内生长更有效,用7g治疗的小鼠在治疗期间的体重增加比5-FU治疗的小鼠更多,表明毒性作用比5-FU低。用7g治疗后,通过H&E染色评估,肿瘤表现出典型的形态学改变。