Synthesis and anticancer evaluation of 3-aryl-6-phenylimidazo[2,1-b]thiazoles |
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| Institution: | 1. Fluoroorganic Division, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India;2. Centre for Chemical Biology, CSIR-Indian Institute of Chemical Technology, Tarnaka, Hyderabad 500007, India;1. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran;2. Department of Medicinal Chemistry and Pharmaceutical Sciences Research Center, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran;3. Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran 14176, Iran;4. Persian Medicine and Pharmacy Research Center, Tehran University of Medical Sciences, Tehran, Iran;5. Department of Medicinal Chemistry, Faculty of Pharmacy, Shahid Sadoughi University of Medical Sciences, Yazd, Iran;6. Neurobiomedical Research Center, School of Medicine, Shahid Sadoughi University of Medical Sciences, Yazd, Iran;1. Egyptian Petroleum Research Institute, Nasr City, P.O. 11727, Cairo, Egypt;2. Department of Chemistry, Faculty of Science, Mansoura University, ET-35516 Mansoura, Egypt;3. The Institute of Scientific and Industrial Research, Osaka University, 8-1 Mihogaoka, Ibaraki-shi, Osaka 567-0047, Japan;1. Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF), Università degli Studi di Palermo, Via Archirafi 32, 90123, Palermo, Italy;2. Dipartimento di Farmacia, Università degli Studi di Salerno, Via G. Paolo II 132, 84084, Fisciano, Salerno, Italy;3. Department of Medical Oncology, VU University Medical Center, Cancer Center Amsterdam, De Boelelaan 1117, 1081HV, Amsterdam, the Netherlands;4. Cancer Pharmacology Lab, AIRC Start-Up Unit, University of Pisa and Fondazione Pisana per la Scienza, via Via Ferruccio Giovannini 13, 56017, San Giuliano Terme, Pisa, Italy |
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| Abstract: | A series of new 3,6-diphenylimidazo2,1-b]thiazole derivatives (4a–l) are synthesized and evaluated for their anticancer activity. Some of the synthesized compounds have shown potent anti-proliferative activity against HeLa, MDA-MB-231, A549 and THP1 human cancer cell lines. Among the active compounds, 3-(3-trifluoromethylphenyl)-6-phenylimidazo2,1-b]thiazole (4j) has caused significant cytotoxicity in HeLa cells, with IC50 as low as 6.5 μM. Compound 4j has induced caspase-3 and caspase-8 activation, leading to an apoptotic cell death. FACS analysis has revealed that compound 4j arrests cells in G0/G1 phase. The presence of 3-(3-trifluoromethylphenyl)- or 3-(3-chlorophenyl)-substituent, in that order, on the 6-phenylimidazo2,1-b]thiazole impacts more positively than other aryl-substituents, on the anti-proliferative properties of these compounds. |
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| Keywords: | Thiazole Anticancer activity Cell cycle effects Caspase assay |
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