NAD(P)H:醌氧化还原酶1(NQO1)专性催化醌两电子还原反应, 具有化学保护和生物激活作用。NQO1 在多种肿瘤细胞特别是肺癌、结肠癌、乳腺癌细胞中的表达远高于正常组织。由于NQO1在肿瘤细胞的高表达及其生物活化的特性, 它被认为是治疗多种肿瘤的潜在分子靶标。靶向 NQO1 药物有望实现高选择性、特异性杀灭肿瘤细胞。本文重点综述了该类化合物构效关系研究, 并提出了新的研究思路, 旨在促进对靶向 NQO1 抗肿瘤醌的研究和开发。 NAD (P) H: Quinone oxidoreductase 1 (NQO1) is a specialized catalytic quinone two-electron reduction reaction with chemical protection and bioactivation. NQO1 expression in many kinds of tumor cells, especially lung cancer, colon cancer and breast cancer cells is much higher than normal tissues. Because of its high expression in tumor cells and its biological activation properties, NQO1 is considered as a potential molecular target for various tumors. Targeted NQO1 drugs are expected to achieve high selectivity and specificity to kill tumor cells. This review focuses on the structure-activity relationship of these compounds and proposes new research ideas aimed at promoting the research and development of anti-tumor quinones targeting NQO1.