释放ZnO-NPs辅助非均相合成的潜力:一种制造融合噻吩吡啶作为前列腺癌治疗支架的新方法

IF 3.7 2区 化学 Q2 CHEMISTRY, APPLIED
Parveen Kumar, Gourav Kumar, Tejveer Singh, Meena Nemiwal
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引用次数: 0

摘要

在此,我们描述了一个有效的多相方案,通过使用不同的噻吩羧醛和甘氨酸酯,通过简单的ZnO纳米颗粒(ZnO- nps)催化,一锅合成融合噻吩吡啶衍生物。这种新方法具有相当大的官能团耐受性,在适当的反应时间内以中等到良好的产率产生目标噻吩吡啶衍生物。ZnO-NPs的催化存在通过增强醛的亲电性和激活羰基,从而促进合成融合噻吩吡啶缀合物的亲核攻击,显著提高了反应效率。在一系列合成的衍生物中,化合物3aa对前列腺癌(PC-3)细胞系和人胚胎肾(HEK)细胞的体外抗癌作用进行了评价。值得注意的是,化合物3aa对PC-3细胞株表现出明显的抑制活性,IC50值为12.7 μM。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Unlocking the Potential of ZnO-NPs Assisted Heterogeneous Synthesis: A Novel Approach to Fabricate Fused Thienopyridines as a Promising Scaffold for Prostate Cancer Treatment

Unlocking the Potential of ZnO-NPs Assisted Heterogeneous Synthesis: A Novel Approach to Fabricate Fused Thienopyridines as a Promising Scaffold for Prostate Cancer Treatment

Herein, we delineate an efficacious heterogeneous protocol for the one-pot synthesis of fused thienopyridine derivatives through the employment of diverse thiophene carboxaldehydes and glycine esters, catalyzed by simple ZnO nanoparticles (ZnO-NPs). This novel methodology exhibits considerable functional group tolerance, yielding the targeted thienopyridine derivatives in moderate to good yield within appropriate reaction time. The catalytic presence of ZnO-NPs significantly enhances reaction efficiency by augmenting the electrophilic nature of aldehydes and activating the carbonyl group, thus facilitating nucleophilic attack for the synthesis of fused thienopyridine conjugates. Within the array of synthesized derivatives, compound 3aa underwent evaluation for its in vitro anticancer efficacy against prostate cancer (PC-3) cell lines and human embryonic kidney (HEK) cells. Remarkably, compound 3aa exhibited substantial inhibitory activity against PC-3 cell lines, achieving an IC50 value of 12.7 μM.

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来源期刊
Applied Organometallic Chemistry
Applied Organometallic Chemistry 化学-无机化学与核化学
CiteScore
7.80
自引率
10.30%
发文量
408
审稿时长
2.2 months
期刊介绍: All new compounds should be satisfactorily identified and proof of their structure given according to generally accepted standards. Structural reports, such as papers exclusively dealing with synthesis and characterization, analytical techniques, or X-ray diffraction studies of metal-organic or organometallic compounds will not be considered. The editors reserve the right to refuse without peer review any manuscript that does not comply with the aims and scope of the journal. Applied Organometallic Chemistry publishes Full Papers, Reviews, Mini Reviews and Communications of scientific research in all areas of organometallic and metal-organic chemistry involving main group metals, transition metals, lanthanides and actinides. All contributions should contain an explicit application of novel compounds, for instance in materials science, nano science, catalysis, chemical vapour deposition, metal-mediated organic synthesis, polymers, bio-organometallics, metallo-therapy, metallo-diagnostics and medicine. Reviews of books covering aspects of the fields of focus are also published.
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