1,2,3-Triazole-Chalcone hybrids: Synthesis, in vitro cytotoxic activity and mechanistic investigation of apoptosis induction in multiple myeloma RPMI-8226

Ashour Heba F.; Abou-zeid Laila A.; El-Sayed Magda A-A; Selim Khalid B.

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1,2,3-Triazole-Chalcone hybrids: Synthesis, in vitro cytotoxic activity and mechanistic investigation of apoptosis induction in multiple myeloma RPMI-8226

机译：1,2,3-三唑 - 氯酮杂交种：合成，体外细胞毒性活性和多发性骨髓瘤凋亡诱导的机械调查RPMI-8226

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A new series of 1,2,3-triazole-chalcone hybrids has been synthesized and screened in vitro against a panel of 60 human cancer cell lines according to NCI (USA) protocol. Compound 4d having 3, 4-dimethoxyphenyl chalcone moiety, the most potent derivative, inhibited the growth of RPMI-8226 and SR leukemia cell lines by 99.73% and 94.95% at 10 mu M, respectively. Also, it inhibited the growth of M14 melanoma, K-562 leukemia, and MCF7 breast cancer cell lines by more than 80% at the same test concentration. 4d showed IC50 values less than 1 mu M on six types of tumor cells and high selectivity index reached to 104 fold on MCF7. Compound 4d showed superior activity than methotrexate and gefitinib against the most sensitive leukemia cell lines in addition to higher or comparable activity against the rest sensitive cell lines. Flow cytometry analysis in RPMI-8226 cells revealed that compound 4d caused cell cycle arrest at G2/M phase and induced apoptosis in a dose dependant manner. Mechanistic evaluation referred this apoptosis induction to triggering mitochondrial apoptotic pathway through inducing ROS accumulation, increasing Bax/Bcl-2 ratio and activation of caspases 3, 7 and 9. Copyright (C) 2020 Elsevier Masson SAS. All rights reserved.

机译：根据NCI（USA）协议，已经合成并筛选了一种新的1,2,3-三唑类杂交杂交体并筛选体外筛选60例人癌细胞系。具有3,4-二甲氧基苯基Cholcone部分，最有效的衍生物，最有效的衍生物，抑制RPMI-8226和Sr白血病细胞系的生长分别在10μm下的99.73％和94.95％。此外，它抑制M14黑素瘤，K-562白血病和MCF7乳腺癌细胞系的生长，在相同的测试浓度下超过80％。图4D显示IC50值小于1μm的肿瘤细胞，并且在MCF7上达到104倍的高选择性指数。除了对静敏细胞系的更高或类似的活性之外，化合物4d表现出比甲氨蝶呤和吉非替尼对甲氨蝶呤和吉非尼菌的优异活性表现出。 RPMI-8226细胞中的流式细胞术分析显示，化合物4D在G2 / M相引起细胞周期停滞，并以剂量依赖性方式诱导细胞凋亡。机械评估通过诱导ROS累积，增加了Bax / Bcl-2比和Caspases 3,7和9的激活来触发线粒体凋亡途径。版权所有（C）2020 Elsevier Masson SAS。版权所有。

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《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2020年第2020期|共14页
作者
Ashour Heba F.; Abou-zeid Laila A.; El-Sayed Magda A-A; Selim Khalid B.;
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Mansoura Univ Fac Pharm Dept Pharmaceut Organ Chem Mansoura 35516 Egypt;

Mansoura Univ Fac Pharm Dept Pharmaceut Organ Chem Mansoura 35516 Egypt;

Mansoura Univ Fac Pharm Dept Pharmaceut Organ Chem Mansoura 35516 Egypt;

Mansoura Univ Fac Pharm Dept Pharmaceut Organ Chem Mansoura 35516 Egypt;

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原文格式 PDF
正文语种 eng
中图分类药学;
关键词
Antiproliferative activity; 1; 2; 3-Triazole; Chalcone; Cell cycle analysis; Apoptosis; ROS; NCI-60;

机译：抗增殖活动;1;2;3-三唑;螯合;细胞循环分析;细胞凋亡;ROS;NCI-60;

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1. 1,2,3-Triazole-Chalcone hybrids: Synthesis, in vitro cytotoxic activity and mechanistic investigation of apoptosis induction in multiple myeloma RPMI-8226 [J] . Ashour Heba F., Abou-zeid Laila A., El-Sayed Magda A-A, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2020,第期

机译：1,2,3-三唑 - 氯酮杂交种：合成，体外细胞毒性活性和多发性骨髓瘤凋亡诱导的机械调查RPMI-8226
2. Design, synthesis, in vitro cytotoxic activity evaluation, and apoptosis-induction study of new 9(10H)-acridinone-1,2,3-triazoles [J] . Mohammadi-Khanaposhtani Maryam, Safavi Maliheh, Sabourian Reyhaneh, Molecular diversity . 2015,第4期

机译：新型9（10H）-ac啶酮-1,2,3-三唑的设计，合成，体外细胞毒性活性评估和凋亡诱导研究
3. Synthesis of newer 1,2,3-triazole linked chalcone and flavone hybrid compounds and evaluation of their antimicrobial and cytotoxic activities [J] . Kant Rama, Kumar Dharmendra, Agarwal Drishti, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2016,第Null期

机译：新型1,2,3-三唑连接的查尔酮和黄酮杂化化合物的合成及其抗微生物和细胞毒性活性的评估
4. The Synthesis of Ethyl-1-Benzyl-5-Methyl-1H-1,2,3-Triazoles-4-Carboxylate Using Microwave Assisted Organic Synthesis Method and Determination of Its Corrosion Inhibition Activity on Carbon Steel [C] . Rayyane Mazaya Syifa Insani, Deana Wahyuningrum, Bunbun Bundjali Materials Research Society of Indonesia Meeting . 2015

机译：使用微波辅助有机合成方法合成乙基-1-苄基-5-甲基-1H-1,2,3-三唑-4-羧酸盐及其对碳钢腐蚀抑制活性的测定
5. 8-Amino-adenosine and induction of apoptosis in multiple myeloma: Effect of novel purine analog on cellular signaling pathways. [D] . Ghias, Kulsoom. 2005

机译：8-氨基腺苷与多发性骨髓瘤细胞凋亡的诱导：新型嘌呤类似物对细胞信号通路的影响。
6. Synthesis Structure and In Vitro Cytotoxic Activity of Novel Cinchona—Chalcone Hybrids with 14-Disubstituted- and 15-Disubstituted 123-Triazole Linkers [O] . Tamás Jernei, Cintia Duró, Antonio Dembo, 2019

机译：具有14-二取代和15-二取代的123-三唑连接基的新型金鸡纳-查尔酮杂种的合成结构和体外细胞毒活性
7. Design and synthesis of pironetin analogue/combretastatin A-4 hybrids containing a 1,2,3-triazole ring and evaluation of their cytotoxic activity [O] . Vilanova Gallén Concepción, Torijano Gutiérrez Sandra Adela, Díaz Oltra Santiago, 2015

机译：设计和合成含有1,2,3-三唑环的pironetin类似物/ combretastatin a-4杂种并评估其细胞毒活性
8. Synthesis, Characterization, and Structural Investigations of 1-amino-3-Substituted- 1,2,3-Triazolium Salts, and a New Route to 1-substituted-1,2,3- triazoles [R] . Kaplan, G. , Drake, G. , Tollison, K. , 2004

机译：1-氨基-3-取代-1,2,3-三唑盐的合成，表征和结构研究，以及1-取代-1,2,3-三唑的新途径

1,2,3-Triazole-Chalcone hybrids: Synthesis, in vitro cytotoxic activity and mechanistic investigation of apoptosis induction in multiple myeloma RPMI-8226

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