Prospecting for cytotoxic and antiprotozoal 4‐aryl‐4 H H ‐chromenes and 10‐aryldihydropyrano[2,3‐ f f ]chromenes

Martin Erlon F.; Mbaveng Armelle T.; de Moraes Milene H.; Kuete Victor; Biavatti Maique W.; Steindel Mario; Efferth Thomas; Sandjo Louis P.

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Prospecting for cytotoxic and antiprotozoal 4‐aryl‐4 H H ‐chromenes and 10‐aryldihydropyrano[2,3‐ f f ]chromenes

机译：细胞毒性和抗丙二醇4-芳基-4H H H H H H H H H H H H H H H H H-Fchromenes [2,3-f]铬

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Abstract Different studies reported that genetic predisposition or metabolic dysfunction are the risk factors for cancer. Infectious parasitic diseases were listed among factors that predispose to cancer. Because of the resemblance between the life cycle of cancer cells and some parasites, this study aimed to prepare pyran derivatives with cytotoxic and antiprotozoal potencies. Therefore, 7 chromenes, 10 pyranocoumarins, and an unexpected intermediate were obtained from a multi‐reagent one‐pot reaction. These compounds were evaluated for their cytotoxicity on sensitive and resistant leukemia cancer cells lines and against two protozoan parasites, namely Trypanosoma cruzi and Leishmania amazonensis amastigote. Promising cytotoxicity (IC 50 values of less than 1?μM) was obtained for two of the synthetic products ( 12 and 15 ). Compound 12 induced apoptosis and cell cycle arrest in CCRF‐CEM leukemia cells in G0/G1 while compound 15 and doxorubicin induced apoptosis and arrest in the S and G2/M phases. Ten of these products showed trypanocidal activity, while only five of them were weakly active on L. amazonensis . Three of the obtained pyrans showed significant cytotoxicity and antitrypanocidal activity, simultaneously. Nevertheless, all antiparasitic compounds revealed potency with low selectivity toward THP‐1 cells used as host.

机译：摘要不同的研究报告称，遗传易感性或代谢功能障碍是癌症的危险因素。在易患癌症的因素中列出了传染性寄生虫病。由于癌细胞生命周期与一些寄生虫之间的相似性，这项研究旨在制备具有细胞毒性和抗双胞痘型疗效的吡喃衍生物。因此，从多试剂单罐反应中获得7种色谱，10种吡喃加洛林和意外中间体。评估这些化合物对敏感和抗性白血病癌细胞系中的细胞毒性，并针对两个原生动物寄生虫，即Trypanosoma Cruzi和Leishmaniaazonensis Amastigote。有希望的细胞毒性（IC 50值小于1？μm），用于两种合成产物（12和15）。化合物12在G0 / G1的CCRF-CEM白血病细胞中诱导细胞凋亡和细胞周期停滞，而化合物15和多柔比蛋白诱导S和G2 / m阶段的凋亡和捕获。这些产品中的十种表现出胰蛋白酶活性，而其中只有五个在L.Amazonensis上略微活跃。其中三种所得吡喃同时显示出显着的细胞毒性和抗酸催化活性。然而，所有抗缺氧素化合物都揭示了朝向作为宿主使用的THP-1细胞的低选择性的效力。

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来源
《Archiv der Pharmazie》 |2018年第10期|共11页
作者
Martin Erlon F.; Mbaveng Armelle T.; de Moraes Milene H.; Kuete Victor; Biavatti Maique W.; Steindel Mario; Efferth Thomas; Sandjo Louis P.;
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作者单位

Department of Pharmaceutical SciencesUniversidade Federal de Santa CatarinaFlorianópolis Brazil;

Faculty of Science Department of BiochemistryUniversity of DschangDschang Cameroon;

Department of Microbiology Immunology and ParasitologyUniversidade Federal de Santa;

Faculty of Science Department of BiochemistryUniversity of DschangDschang Cameroon;

Department of Pharmaceutical SciencesUniversidade Federal de Santa CatarinaFlorianópolis Brazil;

Department of Microbiology Immunology and ParasitologyUniversidade Federal de Santa;

Department of Pharmaceutical Biology Institute of Pharmacy and BiochemistryJohannes Gutenberg;

Department of Pharmaceutical SciencesUniversidade Federal de Santa CatarinaFlorianópolis Brazil;

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中图分类药学;
关键词
4‐aryl‐4 H ‐chromenes; 10‐aryl2; 3‐ f pyranocoumarins; antiprotozoal activity; cell cycle arrest; cytotoxicity;

机译：4-芳基-4h -Chromenes;10-芳基[2;3-F]吡喃替脲;抗曲根活;细胞周期骤停;细胞毒性;

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1. Prospecting for cytotoxic and antiprotozoal 4‐aryl‐4 H H ‐chromenes and 10‐aryldihydropyrano[2,3‐ f f ]chromenes [J] . Martin Erlon F., Mbaveng Armelle T., de Moraes Milene H., Archiv der Pharmazie . 2018,第10期

机译：细胞毒性和抗丙二醇4-芳基-4H H H H H H H H H H H H H H H H H-Fchromenes [2,3-f]铬
2. Microwave-assisted synthesis of 10-aryl-4-methyl-2-oxo-8-phenyl-2,8-dihydropyrano[2,3-f]chromene-9-carbaldehydes by Suzuki coupling and their antimicrobial activity [J] . Ashok Dongamanti, Lakshmi Bommidi Vijaya, Ravi Sidda, Chemistry of heterocyclic compounds . 2015,第5期

机译：铃木偶联微波辅助合成10-芳基-4-甲基-2-甲基-2-氧代-8-苯基-2,8-二氢吡喃并[2,3-f]亚甲基-9-甲醛及其抗菌活性
3. Microwave-assisted synthesis of 8-aryl-10-chloro-4-methyl-2-oxo-2,8-dihydropyrano[2,3-f]chromene-9-carbaldehydes and their antimicrobial activity [J] . Ashok D., Lakshmi B. Vijaya, Ganesh Arram, Russian Journal of General Chemistry . 2014,第11期

机译：微波辅助合成8-芳基-10-氯-4-甲基-2-氧代-2-8-二氢吡喃[2,3-f]亚甲基-9-甲醛及其抑菌活性
4. Effect of chromene unit structure on photochromic and thermochromic properties of chromene-3-carbaldehyde hydrazones [C] . Jana Donovalova, Henrieta Stankovicova, Margita Lacova European Symposium on Organic Chemistry . 2009

机译：铬单元结构对铬 - 3-碳醛腙的光致变色和热致变色特性的影响
5. Simultaneous synthesis of both rings of chromenes via a benzannulation/ortho-quinone methide formation/electrocyclization cascade and an approach towards the asymmetric synthesis of chromenes [D] . Majumdar, Nilanjana 2012

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6. Efficient Catalyst One-Pot Synthesis of 7-(Aryl)-10,10-dimethyl-10,11-dihydrochromeno[4,3-b]chromene-6,8(7H,9H)-dione Derivatives Complemented by Antibacterial Activity [O] . Yasameen K. Al-Majedy, Ahmed A. Al-Amiery, Abdul Amir H. Kadhum, 2006

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7. Synthesis and cytotoxic evaluation of novel chromenes and chromene(2,3-d)pyrimidines [O] . Yousif Mahmoud N. M., El-Gazzar Abdel-Rahman B. A., Fayed Ahmed A., 2020

机译：新型结晶铬（2,3-D）嘧啶的合成和细胞毒性评价

Prospecting for cytotoxic and antiprotozoal 4‐aryl‐4 H H ‐chromenes and 10‐aryldihydropyrano[2,3‐ f f ]chromenes

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