通过无溶剂杂环开发抗癌和抗糖尿病多氢喹啉衍生物

IF 2.1 4区 材料科学 Q3 CHEMISTRY, MULTIDISCIPLINARY Journal of Nanoparticle Research Pub Date : 2024-09-20 DOI:10.1007/s11051-024-06136-7
K. S. Patil, S. T. Mane, S. S. Mohite, D. G. Kanase
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引用次数: 0

摘要

在此,我们开发了一种异相催化剂,用于在无溶剂、温和的温度条件下,通过杂环合成法合成各种抗癌和抗糖尿病的多氢喹啉衍生物。这种方法无需进行复杂的净化或柱层析,从而最大限度地减少了废物的产生。此外,催化剂可以多次回收和重复使用,而不会影响产品的产量,这证明了催化剂的可持续性和环保性。此外,我们还评估了每种合成衍生物的抗癌和抗糖尿病活性。初步测定显示,某些衍生物对人类乳腺癌细胞具有良好的抑制作用,这表明它们具有作为未来抗癌剂先导结构的潜力。此外,还对合成的衍生物进行了抗糖尿病活性评估,结果显示它们具有卓越的疗效。值得注意的是,含有 -H、-CH3 和 -OCH3 取代基的衍生物表现出卓越的抗癌活性,而含有 -H 和 -Br 取代基的衍生物则表现出显著的抗糖尿病活性,突显了它们的治疗潜力。因此,我们的研究为合成多氢喹啉衍生物提供了一种有效且可持续的方法,强调了催化剂在有机合成和药物化学应用中的双重优势。
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Development of anticancer and antidiabetic polyhydroquinoline derivatives by solvent-free heterocyclization

Herein we have developed a heterogeneous catalyst for synthesizing various anticancer and antidiabetic polyhydroquinoline derivatives via heterocyclic synthesis under solvent-free conditions at mild temperatures. This approach eliminates the need for complex cleanup or column chromatography, thus minimizing waste production. Moreover, the catalyst can be recovered and reused up to multiple times without compromising product yields, demonstrating its sustainability and environmental friendliness. Additionally, we evaluated each synthetic derivative for anticancer and antidiabetic activities. Initial assays revealed that certain derivatives exhibit promising inhibition against human breast cancer cells, suggesting their potential as lead structures for future anticancer agents. Furthermore, the synthesized derivatives were assessed for antidiabetic activity, showing superior efficacy. Notably, derivatives containing –H, –CH3, and –OCH3 substituents demonstrated excellent anticancer activity, while derivatives containing –H and –Br substituents showed notable antidiabetic activities, highlighting their therapeutic potential. Thus, our study presents an effective and sustainable approach for synthesizing polyhydroquinoline derivatives, emphasizing the catalyst's dual benefits in organic synthesis and medicinal chemistry applications.

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来源期刊
Journal of Nanoparticle Research
Journal of Nanoparticle Research 工程技术-材料科学:综合
CiteScore
4.40
自引率
4.00%
发文量
198
审稿时长
3.9 months
期刊介绍: The objective of the Journal of Nanoparticle Research is to disseminate knowledge of the physical, chemical and biological phenomena and processes in structures that have at least one lengthscale ranging from molecular to approximately 100 nm (or submicron in some situations), and exhibit improved and novel properties that are a direct result of their small size. Nanoparticle research is a key component of nanoscience, nanoengineering and nanotechnology. The focus of the Journal is on the specific concepts, properties, phenomena, and processes related to particles, tubes, layers, macromolecules, clusters and other finite structures of the nanoscale size range. Synthesis, assembly, transport, reactivity, and stability of such structures are considered. Development of in-situ and ex-situ instrumentation for characterization of nanoparticles and their interfaces should be based on new principles for probing properties and phenomena not well understood at the nanometer scale. Modeling and simulation may include atom-based quantum mechanics; molecular dynamics; single-particle, multi-body and continuum based models; fractals; other methods suitable for modeling particle synthesis, assembling and interaction processes. Realization and application of systems, structures and devices with novel functions obtained via precursor nanoparticles is emphasized. Approaches may include gas-, liquid-, solid-, and vacuum-based processes, size reduction, chemical- and bio-self assembly. Contributions include utilization of nanoparticle systems for enhancing a phenomenon or process and particle assembling into hierarchical structures, as well as formulation and the administration of drugs. Synergistic approaches originating from different disciplines and technologies, and interaction between the research providers and users in this field, are encouraged.
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