基于一锅级联方案的抗肿瘤spirooxindol吡咯烷包埋哌啶酮杂环杂环化合物的区域和立体选择性合成。

Q1 Chemistry
Natarajan Arumugam, Abdulrahman I Almansour, Raju Suresh Kumar, Dhaifallah M Al-Thamili, Govindasami Periyasami, V S Periasamy, Jegan Athinarayanan, Ali A Alshatwi, S M Mahalingam, J Carlos Menéndez
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引用次数: 0

摘要

背景:在[bmim]Br中,通过串联三组分1,3-偶极环加成和随后的烯胺反应,以完整的区域选择性和立体选择性合成了螺吡咯烷系哌啶酮杂环杂环化合物。合成的化合物对FaDu下咽肿瘤细胞的抗肿瘤活性进行了评价。有趣的是,大多数化合物显示出与标准抗癌药物博来霉素相似的细胞毒性,其中两种化合物(5a和5g)的活性略高于参比药物。结论:合成的化合物在癌细胞模型中也被评估了其诱导凋亡的特性,发现用化合物5a-e治疗可导致凋亡细胞死亡。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Regio and stereoselective synthesis of anticancer spirooxindolopyrrolidine embedded piperidone heterocyclic hybrids derived from one-pot cascade protocol.

Background: Spiropyrrolidine tethered piperidone heterocyclic hybrids were synthesized with complete regio- and stereoselectively in excellent yield via a tandem three-component 1,3-dipolar cycloaddition and subsequent enamine reaction in [bmim]Br. The synthesized compounds were evaluated for their anticancer activity against FaDu hypopharyngeal tumor cells.

Findings: Interestingly, most compounds displayed cytotoxicities similar to the standard anticancer agent bleomycin, with two of them (5a and 5g) being slightly more active than the reference drug.

Conclusion: Synthesized compounds have also been evaluated for their apoptosis-inducing properties in a cancer cell model, finding that treatment with compounds 5a-e led to apoptotic cell death.

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来源期刊
Chemistry Central Journal
Chemistry Central Journal 化学-化学综合
CiteScore
4.40
自引率
0.00%
发文量
0
审稿时长
3.5 months
期刊介绍: BMC Chemistry is an open access, peer reviewed journal that considers all articles in the broad field of chemistry, including research on fundamental concepts, new developments and the application of chemical sciences to broad range of research fields, industry, and other disciplines. It provides an inclusive platform for the dissemination and discussion of chemistry to aid the advancement of all areas of research. Sections: -Analytical Chemistry -Organic Chemistry -Environmental and Energy Chemistry -Agricultural and Food Chemistry -Inorganic Chemistry -Medicinal Chemistry -Physical Chemistry -Materials and Macromolecular Chemistry -Green and Sustainable Chemistry
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