Department of Chemistry, Faculty of Science, Atatürk University, Erzurum, Turkey.
Department of Chemistry and Chemical Process Technologies, Erzurum Vocational High School, Atatürk University, Erzurum, Turkey.
J Biomol Struct Dyn. 2022 May;40(8):3525-3550. doi: 10.1080/07391102.2020.1848627. Epub 2020 Nov 17.
A series of new chalcones containing fluoro atom at B ring have been designed, synthesized, and evaluated to be antiproliferative activity against a panel of human tumor cell lines. Some of the analogs (, , , , and ) displayed powerful antiproliferative effects to certain human tumor cells, but all of them were devoid of any cytotoxicity towards the normal HEK 293. Acridine orange staining data supported that the cytotoxic and antiproliferative effects of the synthesized analogs on tumor cells are mediated through apoptosis. The compounds and manifested concentration-dependent antiproliferative activity in human hepatocellular carcinoma cell lines using an xCELLigence assay. The structures and antiproliferative activity relationship were further supported by in silico molecular docking study of the compounds against tubulin protein which suggests our compounds interference to cell division. Communicated by Ramaswamy H. Sarma.
设计、合成并评价了一系列新型含氟原子 B 环查尔酮，以评估其对一系列人肿瘤细胞系的抗增殖活性。部分类似物（、、、、和）对某些人肿瘤细胞表现出强大的抗增殖作用，但它们对正常 HEK 293 均无任何细胞毒性。吖啶橙染色数据支持合成类似物对肿瘤细胞的细胞毒性和抗增殖作用是通过细胞凋亡介导的。化合物和在使用 xCELLigence 测定法的人肝癌细胞系中表现出浓度依赖性的抗增殖活性。化合物与微管蛋白蛋白的计算机分子对接研究进一步支持了结构和抗增殖活性关系，这表明我们的化合物对细胞分裂有干扰作用。通讯作者为 Ramaswamy H. Sarma。
