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新型查尔酮结合结构修饰的吡啶 - 嘧啶衍生物作为抗癌剂:其设计、合成及体外评价

New Chalcone Incorporated Structurally Modified Pyridine-Pyrimidine Derivatives as Anticancer Agents: Their Design, Synthesis, and in-vitro Evaluation.

作者信息

Ketha Swarupa, Sudhakar Chithaluri, Kethireddy Shashikala, Eppakayala Laxminarayana

机构信息

Department of Chemistry, GITAM Deemed to be University, Patancheru, Hyderabad 502329, Telangana, India.

Geethanjali College of Engineering and Technology, Keesara, Rangareddy 501301, Telangana, India.

出版信息

Chem Biodivers. 2024 Dec;21(12):e202401122. doi: 10.1002/cbdv.202401122. Epub 2024 Oct 22.

Abstract

Chalcone-incorporated pyridine-pyrimidines i.e. derivatives of (5-(6-(pyrimidin-5-yl)pyridin-3-yl)thiophen-2-yl)prop-2-en-1-one were synthesized and their structures were confirmed by analytical techniques. In addition, all the derivatives were examined for their capacity to fight against cancer towards four cell lines, including breast (MCF-7), prostate (DU-145 and PC3), and lung (A549) by utilizing the MTT technique and the clinically used chemotherapy medication, etoposide serving as a positive reference. All these results were expressed in IC μM, and values of synthesized compounds are compared with a reference drug, showing values ranging from 1.97±0.45 μM to 3.08±0.135 μM. Among those, a few compounds 10(a-e) demonstrated strong activities with corresponding cell lines.

摘要

合成了含查尔酮的吡啶 - 嘧啶,即(5-(6-(嘧啶 - 5 - 基)吡啶 - 3 - 基)噻吩 - 2 - 基)丙 - 2 - 烯 - 1 - 酮的衍生物,并通过分析技术确认了它们的结构。此外,利用MTT技术检测了所有衍生物对四种癌细胞系(包括乳腺癌(MCF - 7)、前列腺癌(DU - 145和PC3)和肺癌(A549))的抗癌能力,临床使用的化疗药物依托泊苷作为阳性对照。所有这些结果均以IC μM表示,并将合成化合物的值与参考药物进行比较,显示值范围为1.97±0.45 μM至3.08±0.135 μM。其中,一些化合物10(a - e)对相应的细胞系表现出较强的活性。

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