1309935-24-7Relevant articles and documents
Synthesis and antitumor activity of 5-[1-(3-(dimethylamino)propyl)-5- halogenated-2-oxoindolin-(3Z)-ylidenemethyl]-2,4-dimethyl-1H-pyrrole-3- carboxamides
Lv, Kai,Wang, Li-Li,Liu, Ming-Liang,Zhou, Xin-Bo,Fan, Shi-Yong,Liu, Hong-Ying,Zheng, Zhi-Bing,Li, Song
, p. 3062 - 3065 (2011/06/24)
We report herein the design and synthesis of novel 1-[3-(dimethylamino) propyl]indolin-2-one derivatives based on the structural features of Sunitinib, a known multitargeted receptor tyrosine kinase inhibitor, and TMP-20, a previously discovered compound with good antitumor activity in our lab. These newly synthesized derivatives were evaluated for in vitro activity against five human cancer cell lines and VEGF/bFGF-stimulated HUVECs. Results revealed that all of the target compounds 1a-p show potent antitumor activity, compounds 1e-h (IC50's: 0.45-5.08 μM) are more active than Sunitinib (IC 50's: 1.35-6.61 μM), and the most active compound 1h (IC 50: 0.47-3.11 μM) is 2.1-4.6-fold more potent than Sunitinib against all five cancer cell lines. In addition, like Sunitinib, 1a-p have higher selectivity on VEGF-stimulated HUVEC other than bFGF-stimulated HUVEC.