A series of novel indolizinophthalazine-5,12-dione derivatives were designed and synthesized by the reaction of 6,7-dichlorophthalazine-5,8-dione with active methylene reagents (AMR) and pyridine derivatives. Some of synthesized compounds exhibited significant in vitro antiproliferative activity at micromolar level toward four human tumor cell lines, including lung adenocarcinoma cell, large-cell lung carcinoma cell, breast carcinoma cell and ardriamycin-resistance breast carcinoma cell. The DNA topoisomerase IB inhibitory assay indicated that DNA topoisomerase IB might be a biological target of the synthesized compounds.

中文翻译：

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吲哚izinophthalazine-5,12-dione衍生物，DNA拓扑异构酶IB抑制剂的合成及其抗增殖活性

通过6,7-二氯邻苯二甲酸-5,8-二酮与活性亚甲基试剂（AMR）和吡啶衍生物的反应，设计合成了一系列新型的吲哚并邻苯二甲酸-5,12-二酮衍生物。一些合成的化合物在微摩尔水平上对四种人类肿瘤细胞系表现出显着的体外抗增殖活性，所述四种人类肿瘤细胞系包括肺腺癌细胞，大细胞肺癌细胞，乳腺癌细胞和耐阿霉素的乳腺癌细胞。DNA拓扑异构酶IB抑制试验表明，DNA拓扑异构酶IB可能是合成化合物的生物学靶标。