基于喹啉并苯并恶嗪自组装模型的新型拓扑异构酶II抑制剂的设计
Design of new topoisomerase II inhibitors based upon a quinobenzoxazine self-assembly model.
作者信息
Zeng Q, Kwok Y, Kerwin S M, Mangold G, Hurley L H
机构信息
Drug Dynamics Institute and Division of Medicinal Chemistry, College of Pharmacy, The University of Texas at Austin, Austin, Texas 78712-1074, USA.
出版信息
J Med Chem. 1998 Oct 22;41(22):4273-8. doi: 10.1021/jm980265c.
A new class of pyridobenzophenoxazine compounds has been developed as topoisomerase II inhibitors for anticancer chemotherapy. These compounds were designed based on a proposed model of a quinobenzoxazine self-assembly complex on DNA. They showed excellent inhibitory effects on several tumor cell lines with nanomolar IC50 values. Their cytotoxic potency correlates with their ability to unwind DNA and inhibit topoisomerase II.
一类新型的吡啶并苯并恶嗪化合物已被开发用作抗癌化疗的拓扑异构酶II抑制剂。这些化合物是基于喹喔啉嗪在DNA上的自组装复合物模型设计的。它们对几种肿瘤细胞系表现出优异的抑制作用，IC50值为纳摩尔级别。它们的细胞毒性效力与其解开DNA和抑制拓扑异构酶II的能力相关。
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