新型拓扑异构酶II导向的双蒽环类类似物的合成、DNA损伤及细胞毒性特性
Synthesis, DNA-damaging and cytotoxic properties of novel topoisomerase II-directed bisantrene analogues.
作者信息
Zagotto G, Oliva A, Guano F, Menta E, Capranico G, Palumbo M
机构信息
Department of Pharmaceutical Sciences, University of Padova, Italy.
出版信息
Bioorg Med Chem Lett. 1998 Jan 20;8(2):121-6. doi: 10.1016/s0960-894x(97)10207-4.
PMID:9871638
Abstract
New bisantrene analogues were synthesized, bearing one or two 4,5-dihydro-1H-imidazol-2-yl hydrazone side chains at positions 1,4 or 9 of the anthracene ring system. A 10-azabioisostere was also prepared. The position of substituents in structurally isomeric drugs modulates topoisomerase II poisoning and specificity, along with cytotoxicity.
摘要
合成了新的双膦三烯类似物，在蒽环系统的1、4或9位带有一个或两个4,5-二氢-1H-咪唑-2-基腙侧链。还制备了一种10-氮杂生物电子等排体。结构异构体药物中取代基的位置调节拓扑异构酶II中毒和特异性以及细胞毒性。
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