Synthesis and biological evaluation of novel analogues of batracylin with synthetic amino acids and adenosine: an unexpected effect on centromere segregation in tumor cells through a dual inhibition of topoisomerase IIα and Aurora B

Wioleta Januchta; Marcin Serocki; Krystyna Dzierzbicka; Grzegorz Cholewinski; Monika Gensicka; Andrzej Skladanowski

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Synthesis and biological evaluation of novel analogues of batracylin with synthetic amino acids and adenosine: an unexpected effect on centromere segregation in tumor cells through a dual inhibition of topoisomerase IIα and Aurora B

机译：用合成氨基酸和腺苷的新乳蛋白新型类似物的合成与生物学评价：通过拓扑异构酶IIα和极光B的双重抑制对肿瘤细胞Centromere偏析的意外效果

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In the search for new anticancer agents we designed and synthesized batracylin derivatives with linking synthetic amino acid side chains of different lengths and adenosine. Unexpectedly, we have found that in water and the culture media adenosine–amino acid–BAT conjugates form supramolecular structures and this prevents these compounds from entering cells. Consequently, these compounds exerted no biological activity when tested towards two human cell lines, lung adenocarcinoma (A549) and human leukemia (HL-60). In contrast, several amino acid–BAT precursors showed up to 25-fold enhanced cytotoxic activity compared to BAT and these compounds strongly interfered with DNA topoisomerase II activity and its cellular functions. In particular, these conjugates inhibited centromere segregation during mitosis in drug-treated tumor cells by preventing topoisomerase II-dependent Aurora B activation.

机译：在寻找新的抗癌剂，我们设计和合成的肉肉蛋白衍生物，其具有连接的不同长度和腺苷的合成氨基酸侧链。出乎意料的是，我们发现在水和培养介质腺苷 - 氨基酸 - 蝙蝠缀合物形成超分子结构，这可以防止这些化合物进入细胞。因此，当朝向两种人细胞系，肺腺癌（A549）和人白血病（HL-60）测试时，这些化合物没有生物活性。相比之下，与蝙蝠相比，几种氨基酸-BAT前体显示出高达25倍的细胞毒性活性，并且这些化合物强烈干扰DNA拓扑异构酶II活性及其细胞功能。特别地，这些缀合物通过预防拓扑异构酶II依赖性极光B活化来抑制药物处理的肿瘤细胞中的细胞分子中的焦粒子偏析。

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《RSC Advances》 |2016年第49期|共13页
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Wioleta Januchta; Marcin Serocki; Krystyna Dzierzbicka; Grzegorz Cholewinski; Monika Gensicka; Andrzej Skladanowski;
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1. Synthesis and biological evaluation of novel analogues of batracylin with synthetic amino acids and adenosine: an unexpected effect on centromere segregation in tumor cells through a dual inhibition of topoisomerase II alpha and Aurora B [J] . Januchta Wioleta, Serocki Marcin, Dzierzbicka Krystyna, RSC Advances . 2016,第49期

机译：用合成氨基酸和腺苷的蜡蛋白新型类似物的合成与生物学评价：通过拓扑异构酶IIα和极光B的双重抑制对肿瘤细胞Centromere偏析的意外效果
2. Antitumor agents. Part 186: Synthesis and biological evaluation of demethylcolchiceinamide analogues as cytotoxic DNA topoisomerase II inhibitors. [J] . Guan J, Zhu XK, Tachibana Y, Bioorganic and medicinal chemistry . 1998,第11期

机译：抗肿瘤药。第186部分：作为细胞毒性DNA拓扑异构酶II抑制剂的去甲基colchiceinamide类似物的合成和生物学评估。
3. Antitumor agents. 185. Synthesis and biological evaluation of tridemethylthiocolchicine analogues as novel topoisomerase II inhibitors. [J] . Guan J, Zhu XK, Tachibana Y, Journal of Medicinal Chemistry . 1998,第11期

机译：抗肿瘤药。 185.三脱甲基硫代秋水仙碱类似物作为新型拓扑异构酶II抑制剂的合成和生物学评估。
4. New antitumoral cyclic astin analogues containing uncoded amino acid residues:synthesis,structural and biological studies [C] . Filomena Rossi, Giancarlo Zanotti, Michele Saviano, European Peptide Symposium . 2002

机译：含有未编码氨基酸残基的新抗肿瘤患者类似物：合成，结构和生物学研究
5. Design and synthesis of molecular probes to modulate cell membrane permeation: I. Design, synthesis, and biological evaluation of novel chicoric acid analogues as inhibitors of HIV-1 integrase. II. Design, synthesis, and biological evaluation of novel estradiol analogues targeting the membrane estrogen receptor. [D] . Charvat, Trevor Thomas. 2004

机译：设计和合成的分子探针，可调节细胞膜的渗透性：I.设计，合成和生物评价作为抗HIV-1整合酶抑制剂的新型菊苣酸类似物。二。针对膜雌激素受体的新型雌二醇类似物的设计，合成和生物学评估。
6. Synthetic structural and biological studies of the ubiquitin system: synthesis and crystal structure of an analogue containing unnatural amino acids. [O] . S G Love, T W Muir, R Ramage, 1997

机译：泛素系统的合成结构和生物学研究：包含非天然氨基酸的类似物的合成和晶体结构。
7. Synthesis and biological evaluation of novel analogues of batracylin with synthetic amino acids and adenosine: an unexpected effect on centromere segregation in tumor cells through a dual inhibition of topoisomerase IIα and Aurora B [O] . Wioleta Januchta, Marcin Serocki, Krystyna Dzierzbicka, 2016

机译：用合成氨基酸和腺苷的新乳蛋白新型类似物的合成与生物学评价：通过拓扑异构酶IIα和极光B的双重抑制对肿瘤细胞Centromere偏析的意外效果
8. Inhibition of topoisomerase II(alpha) activity in CHO K1 cells by 2-((aminopropyl)amino)ethanethiol (WR-1065). [R] . Grdina, D. J., Constantinou, A., Shigematsu, N., 1993

机译：通过2 - （（氨基丙基）氨基）乙硫醇（WR-1065）抑制CHO K1细胞中的拓扑异构酶II（α）活性。

Synthesis and biological evaluation of novel analogues of batracylin with synthetic amino acids and adenosine: an unexpected effect on centromere segregation in tumor cells through a dual inhibition of topoisomerase IIα and Aurora B

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