129655-21-6

129655-21-6结构式

中文名	比折来新
英文名	1,3-bis[2-[(8S)-8-(chloromethyl)-4-hydroxy-1-methyl-7,8-dihydro-3H-pyrrolo[3,2-e]indole-6-carbonyl]-1H-indol-5-yl]urea
英文别名	1,3-Bis[2-[[[(8S)-8β-chloromethyl-3,6,7,8-tetrahydro-4-hydroxy-1-methylbenzo[1,2-b:4,3-b']dipyrrol]-6-yl]carbonyl]-1H-indol-5-yl]urea BIZELESIN (8S,8'S)-6,6'-[Cbonylbis(iMino-1H- indole-5,2-diylcbonyl)]bis[8-(chloroMethyl)-3,6,7,8-tetrahydro-1-Methylbe N,N'-Bis[2-[[(1S)-1-(chloroMethyl)-1,6-dihydro-5-hydroxy-8-Methylbenzo[1,2-b:4,3-b']dipyrrol-3(2H)-yl]carbonyl]-1H-indol-5-yl]urea NSC-615291 Benzo(1,2-b:4,3-b')dipyrrol-4-ol,6,6'-(carbonylbis(imino-1H-indole-5,2-diylcarbonyl))bis(8-(chloromethyl)-3,6,7,8-tetrahydro-1-methyl-,(S-(R,R)) U-77,779 Bizelesin (USAN/INN) U-77779 Urea, N,N'-bis[2-[[(1S)-1-(chloromethyl)-1,6-dihydro-5-hydroxy-8-methylbenzo[1,2-b:4,3-b']dipyrrol-3(2H)-yl]carbonyl]-1H-indol-5-yl]

描述	Bizelesin(NSC 615291；U-77779)是一种AT特异性DNA烷化剂,可产生DNA链间交联,有效抑制DNA复制,并具有潜在的抗癌活性[1]。
相关类别	研究领域 >> 癌症信号通路 >> 细胞周期/DNA损伤 >> DNA烷基化剂/交联剂
体外研究	Bizelesin(0-5μM,4小时)可以通过靶向人类癌细胞 CEM公司细胞中富含在的脱氧核糖核酸域,造成脱氧核糖核酸特异性损伤,进而造成癌细胞损伤,具有潜在的癌症治疗潜力[1]。比泽莱辛(0-500 nM)在平衡计分卡-1细胞中,当浓度为 10纳米时导致 50%的脱氧核糖核酸合成抑制,相比之下,浓度为 160纳米时才抑制 50%RNA合成,而浓度高达至 200纳米时也没有观察到蛋白质合成的抑制[2]。
参考文献	[1]. J M Woynarowski, et al. AT-rich islands in genomic DNA as a novel target for AT-specific DNA-reactive antitumor drugs. J Biol Chem. 2001 Nov 2;276(44):40555-66. [2]. J M Woynarowski, et al. Effects of bizelesin (U-77,779), a bifunctional alkylating minor groove binder, on replication of genomic and simian virus 40 DNA in BSC-1 cells. Biochim Biophys Acta. 1997 Jul 17;1353(1):50-60.