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1,3,4-oxadiazole/chalcone hybrids: Design, synthesis, and inhibition of leukemia cell growth and EGFR, Src, IL-6 and STAT3 activities.
Bioorganic Chemistry ( IF 5.1 ) Pub Date : 2018-11-22 , DOI: 10.1016/j.bioorg.2018.11.032
Marwa Ali A Fathi 1 , Amer Ali Abd El-Hafeez 2 , Dalia Abdelhamid 1 , Samar H Abbas 1 , Monica M Montano 3 , Mohamed Abdel-Aziz 1
Affiliation  

A new series of 1,3,4-oxadiazole/chalcone hybrids was designed, synthesized, identified with different spectroscopic techniques and biologically evaluated as inhibitors of EGFR, Src, and IL-6. The synthesized compounds showed promising anticancer activity, particularly against leukemia, with 8v being the most potent. The synthesized compounds exhibited strong to moderate cytotoxic activities against K-562, KG-1a, and Jurkat leukemia cell lines in MTT assays. Compound 8v showed the strongest cytotoxic activity with IC50 of 1.95 µM, 2.36 µM and 3.45 µM against K-562, Jurkat and KG-1a leukemia cell lines, respectively. Moreover; the synthesized compounds inhibited EGFR, Src, and IL-6. Compound 8v was most effective at inhibiting EGFR (IC50 = 0.24 μM), Src (IC50 = 0.96 μM), and IL-6 (% of control = 20%). Additionally, most of the compounds decreased STAT3 activation.

中文翻译:

1,3,4-恶二唑/查耳酮杂种:设计,合成和抑制白血病细胞生长以及EGFR,Src,IL-6和STAT3活性。

设计,合成,使用不同的光谱技术鉴定了一系列新的1,3,4-恶二唑/查耳酮杂化物,并对其进行了生物学评估,认为它们是EGFR,Src和IL-6的抑制剂。合成的化合物显示出有希望的抗癌活性,尤其是针对白血病,最有效的是8v。在MTT分析中,合成的化合物对K-562,KG-1a和Jurkat白血病细胞系表现出强至中等的细胞毒活性。化合物8v对K-562,Jurkat和KG-1a白血病细胞株表现出最强的细胞毒活性,IC50分别为1.95 µM,2.36 µM和3.45 µM。而且; 合成的化合物可抑制EGFR,Src和IL-6。化合物8v最有效地抑制EGFR(IC50 = 0.24μM),Src(IC50 = 0.96μM)和IL-6(对照%= 20%)。此外,
更新日期:2018-11-22
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