Heteroaryl substituted ansa-titanocene anti-cancer drugs derived from fulvenes and titanium dichloride

被引:74
作者
Rehmann, FJK
Cuffe, LP
Mendoza, O
Rai, DK
Sweeney, N
Strohfeldt, K
Gallagher, WM
Tacke, M
机构
[1] Univ Coll Dublin, Dept Chem, CSCB, Dublin 4, Ireland
[2] Univ Coll Dublin, Dept Pharmacol, Dublin 4, Ireland
关键词
anti-cancer drug; cis-platinum; titanocene; fulvene; LLC-PK; DFT calculations;
D O I
10.1002/aoc.864
中图分类号
O69 [应用化学];
学科分类号
081704 ;
摘要
Starting from 2-furylfulvene (la), 2-thiophenylfulvene (1b), and 1-methyl-2-pyrrolylfulvene (1c), [1,2di(cyclopentadienyl)-1,2-di-(2-furyl)ethanediyl] titanium dichloride (2a), [1,2-di(cyclopentadienyl)1,2-di-(2-thiophenyl)ethanediyl] titanium dichloride (2b), and [1,2-di(cyclopentadienyl)-1,2-bis-(1methyl-2-pyrrolyl)ethanediyl] titanium dichloride (2c) were synthesized. When titanocenes (2a-c) were tested against pig kidney carcinoma cells (LLC-PK), inhibitory concentrations (50%) of 4.5 x 10(-4) M, 2.9 x 10(-4) M and 2.0 x 10(-4) M respectively were observed. Copyright (c) 2005 John Wiley & Sons, Ltd.
引用
收藏
页码:293 / 300
页数:8
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