1,3,4-oxadiazole/chalcone hybrids: Design, synthesis, and inhibition of leukemia cell growth and EGFR, Src, IL-6 and STAT3 activities.

ABSTRACT: 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??M), Src (IC50?=?0.96??M), and IL-6 (% of control?=?20%). Additionally, most of the compounds decreased STAT3 activation.

SUBMITTER: Fathi MAA 

PROVIDER: S-EPMC6923798 | biostudies-literature | 2019 Mar

REPOSITORIES: biostudies-literature