Synthesis and antiproliferative activity of indolizinophthalazine-5,12-dione derivatives, DNA topoisomerase IB inhibitors.

Shen DQ; Wu ZP; Wu XW; An ZY; Bu XZ; Gu LQ; Huang ZS; An LK

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Synthesis and antiproliferative activity of indolizinophthalazine-5,12-dione derivatives, DNA topoisomerase IB inhibitors.

机译：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。

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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.

机译：通过6,7-二氯酞嗪-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吲哚并嗪-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抑制分析表明DNA拓扑异构酶IB可能是合成化合物的生物学目标。

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《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2010年第9期|共5页
作者
Shen DQ; Wu ZP; Wu XW; An ZY; Bu XZ; Gu LQ; Huang ZS; An LK;
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正文语种 eng
中图分类医药、卫生;劳动卫生;
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1. Synthesis and antiproliferative activity of indolizinophthalazine-5,12-dione derivatives, DNA topoisomerase IB inhibitors. [J] . Shen DQ, Wu ZP, Wu XW, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2010,第9期

机译：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。
2. Synthesis of Methoxy-, Methylenedioxy-, Hydroxy-, and Halo-Substituted Benzophenanthridinone Derivatives as DNA Topoisomerase IB (TOP1) and Tyrosyl-DNA Phosphodiesterase 1 (TDP1) Inhibitors and Their Biological Activity for Drug-Resistant Cancer [J] . Hu De-Xuan, Tang Wen-Lin, Zhang Yu, Journal of Medicinal Chemistry . 2021,第11期

机译：作为DNA拓扑异构酶IB（TOP1）和酪氨酸-DNA磷酸二磷苯氨酯酶1（TDP1）抑制剂及其对耐药性癌症的生物活性的合成甲氧基，亚甲基 - ，羟基苯蒽酮衍生物及其生物活性
3. Synthesis, cytotoxic activities and structure-activity relationships of topoisomerase I inhibitors: indolizinoquinoline-5,12-dione derivatives. [J] . Cheng Y, An LK, Wu N, Bioorganic and medicinal chemistry . 2008,第8期

机译：拓扑异构酶I抑制剂的合成，细胞毒活性和构效关系：吲哚并喹啉5,12-二酮衍生物。
4. Synthesis and Antiproliferative activities of Novel 2-Phenylaminopyrimidine (PAP) Derivatives [C] . Sheng Chang International Conference on Materials and Products Manufacturing Technology . 2014

机译：新型2-苯基氨基嘧啶（PAP）衍生物的合成与抗增殖活性
5. Structural and solution determinants of DNA intercalation and topoisomerase IB inhibition by flavonoids. [D] . Webb, Michael Rene. 2004

机译：类黄酮对DNA嵌入和拓扑异构酶IB抑制的结构和溶液决定因素。
6. Treatment with inhibitors of polyamine biosynthesis which selectively lower intracellular spermine does not affect the activity of alkylating agents but antagonizes the cytotoxicity of DNA topoisomerase II inhibitors. [O] . M. A. Desiderio, D. Bergamaschi, E. Mascellani, 1997

机译：用多胺生物合成抑制剂（选择性降低细胞内精胺）的处理不会影响烷基化剂的活性但会拮抗DNA拓扑异构酶II抑制剂的细胞毒性。
7. Discovery, Synthesis, and Evaluation of Oxynitidine Derivatives as Dual Inhibitors of DNA Topoisomerase IB (TOP1) and Tyrosyl-DNA Phosphodiesterase 1 (TDP1), and Potential Antitumor Agents [O] . -1

机译：氧荷衍生物作为DNA拓扑异构酶IB（TOP1）和酪氨酰-DNA磷酸二酯酶1（TDP1）的双抑制剂的发现，合成和评估和评价，以及潜在的抗肿瘤剂

Synthesis and antiproliferative activity of indolizinophthalazine-5,12-dione derivatives, DNA topoisomerase IB inhibitors.

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