1,3,4-oxadiazole/chalcone hybrids: Design,synthesis, and inhibition of leukemia cell growth and EGFR,Src, IL-6 and STAT3 activities |
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| Institution: | 1. Medicinal Chemistry Department, Faculty of Pharmacy, Minia University, Minia 61519, Egypt;2. Pharmacology and Experimental Oncology Unit, Cancer Biology Department, National Cancer Institute, Cairo University, Cairo 11796, Egypt;3. Pharmacotherapy Department, Graduate School of Biomedical and Health Sciences, Hiroshima University, Hiroshima 734-8553, Japan;4. Pharmacology Department, Case Western Reserve University School of Medicine, 10900 Euclid Avenue, Cleveland, OH 44106, USA;1. Institute of Medicinal Biotechnology, Chinese Academy of Medical Science and Peking Union Medical College, Beijing 100050, China;2. New Drug Research & Development Center, North China Pharmaceutical Group Corporation, Shijiazhuang 050015, China;1. Institute of Oncology and Radiology of Serbia, Pasterova 14, 11000 Belgrade, Serbia;2. Faculty of Science, Department of Chemistry, University of Kragujevac, R. Domanovica 12, 34000 Kragujevac, Serbia;3. Laboratory for Radiobiology and Molecular Genetics, “Vin?a” Institute of Nuclear Sciences, University of Belgrade, 11000 Belgrade, Serbia;4. Faculty of Pharmacy, Department of Organic Chemistry, University of Belgrade, Vojvode Stepe 450, 11221 Belgrade, Serbia;1. The Guangdong Province Key Laboratory of Chemical Biology, The Graduate School at Shenzhen, Tsinghua University, Shenzhen 518055, PR China;2. National & Local United Engineering Lab for Personalized Antitumor Drugs, The Graduate School at Shenzhen, Tsinghua University, Shenzhen 518055, PR China;3. Bioinformatics and Drug Design Group, Department of Pharmacy, Centre for Computational Science and Engineering, 117543, Singapore;4. School of Medicine, Tsinghua University, Beijing 100084, PR China;1. School of Basic Medical Science, Zhengzhou University, Zhengzhou 450001, China;2. School of Pharmaceutical Sciences & Collaborative Innovation Center of New Drug Research and Safety Evaluation, Zhengzhou University, Zhengzhou 450001, China;3. Department of Gastroenterology, The Fifth Affiliated Hospital of Zhengzhou University, Zhengzhou 450052, China;4. Department of Urology, University of California, Irvine, Orange, CA 92868, USA;1. Organic Synthesis and Process Chemistry Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, India;2. Academy of Scientific and Innovative Research (AcSIR), Ghaziabad 201002, India;3. Applied Biology Division, CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, India;4. Department of Genetics, Osmania University, Hyderabad 500007, India;5. School of Pharmaceutical Education and Research, Jamia Hamdard University, New Delhi 110062, India |
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| 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 μM), Src (IC50 = 0.96 μM), and IL-6 (% of control = 20%). Additionally, most of the compounds decreased STAT3 activation. |
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| Keywords: | Leukemia Oxadiazole Chalcone Tyrosine kinases Cytokines STAT3 |
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