作为具有潜在抗癌作用的细胞凋亡诱导剂的 2-(4-((1,3-二氧代异吲哚啉-2-基)甲基)苯基)-N-苯基噻唑-4-甲酰胺衍生物的合成与细胞毒性评估

IF 1.1 4区 化学 Q4 BIOCHEMISTRY & MOLECULAR BIOLOGY
Leila Hosseinzadeh, Ghazal Mahmoudi, Masoumeh Mahsa Mohammadi, Amin Hosseini, Hossein Malekshahi, Alireza Aliabadi
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引用次数: 0

摘要

研究目的为发现新的抗肿瘤药物而进行的癌症化疗是医学和制药研究的最新领域之一。研究方法在本项目中,合成了一系列新型 1,3-噻唑衍生物,并使用三种癌细胞株通过 MTT 试验评估了其相应的抗癌活性。A2780(卵巢癌)、PC3(前列腺癌)和 MCF-7(乳腺癌)被用于此目的。随后,还对一些选定的活性化合物的 Caspase-3 激活、线粒体膜电位(MMP)和活性氧(ROS)生成进行了研究。结果与讨论幸运的是,与其他细胞系相比,测试化合物对 MCF-7 细胞具有很强的活性。化合物(VI)、(VII)、(VIII)、(IX)和(XII)增强了 MCF-7 细胞系中 Caspases-3 的活性,其中 3-Cl 类似物(VII)对 MCF-7 细胞的细胞毒性指数最高。而在上述类似物(VI-IX)和(XII)中,仅有 2-F 衍生物(IV)和(XII)能显著降低线粒体膜电位(MMP)。与其他噻唑衍生物相比,目前的化合物具有更好的抗癌活性。一般来说,带有电子吸收基团和电子供能基团的衍生物对癌细胞株都有活性。结论本文介绍的新型 1,3-噻唑衍生物可作为潜在的抗癌剂,尤其是针对乳腺癌。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Synthesis and Cytotoxicity Evaluation of 2-(4-((1,3-Dioxoisoindolin-2-yl)methyl)phenyl)-N-phenyl-thiazole-4-carboxamide Derivatives as Apoptosis Inducers with Potential Anticancer Effects

Synthesis and Cytotoxicity Evaluation of 2-(4-((1,3-Dioxoisoindolin-2-yl)methyl)phenyl)-N-phenyl-thiazole-4-carboxamide Derivatives as Apoptosis Inducers with Potential Anticancer Effects

Objective: Cancer chemotherapy for the discovery of new antineoplastic drugs is one of the updated areas of medical and pharmaceutical research. Methods: In the current project, a novel series of 1,3-thiazole derivatives were synthesized and their corresponding anticancer activity was evaluated by MTT assay using three cancer cell lines. A2780 (ovarian cancer), PC3 (prostatic carcinoma), and MCF-7 (breast cancer) were utilized for this purpose. Subsequently, Caspase-3 activation, mitochondrial membrane potential (MMP), and generation of reactive oxygen species (ROS) were also explored for some selected active compounds. Results and Discussion: Fortunately, tested compounds were so active against MCF-7 cells compared to other cell lines. Compounds (VI), (VII), (VIII), (IX), and (XII) enhanced Caspases-3 activity in the MCF-7 cell line that 3-Cl analog (VII) was illustrated as the most cytotoxic index against MCF-7 cells. This is while that among the above analogs (VI–IX), and (XII), just and just, 2-F derivative (IV) revealingly reduced the mitochondrial membrane potential (MMP). The current compounds demonstrated better anticancer activity compared to the other thiazole derivatives. Generally, derivatives bearing electron-withdrawing as well as electron-donating groups are active toward cancerous cell lines. Conclusions: The novel 1,3-thiazole derivatives presented in the current paper could be suggested as potential anticancer agents, especially against breast cancer.

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来源期刊
Russian Journal of Bioorganic Chemistry
Russian Journal of Bioorganic Chemistry 生物-生化与分子生物学
CiteScore
1.80
自引率
10.00%
发文量
118
审稿时长
3 months
期刊介绍: Russian Journal of Bioorganic Chemistry publishes reviews and original experimental and theoretical studies on the structure, function, structure–activity relationships, and synthesis of biopolymers, such as proteins, nucleic acids, polysaccharides, mixed biopolymers, and their complexes, and low-molecular-weight biologically active compounds (peptides, sugars, lipids, antibiotics, etc.). The journal also covers selected aspects of neuro- and immunochemistry, biotechnology, and ecology.
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