Imidazopyridine linked triazoles as tubulin inhibitors,effectively triggering apoptosis in lung cancer cell line |
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| Affiliation: | 1. Medicinal Chemistry and Pharmacology Division, CSIR – Indian Institute of Chemical Technology, Hyderabad 500007, India;2. Academy of Scientific and Innovative Research (AcSIR), CSIR – Indian Institute of Chemical Technology, Hyderabad 500007, India;3. School of Pharmaceutical Education and Research, Jamia Hamdard University, New Delhi 110062, India;4. Department of Crop Protection Chemicals, CSIR – Indian Institute of Chemical Technology, Hyderabad 500007, India;1. Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, PR China;2. Center of Drug Discovery, State Key Laboratory of Natural Medicines, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, PR China;3. High Magnetic Field Laboratory, Chinese Academy of Sciences, P.O. Box 1110, Hefei, Anhui 230031, PR China;4. University of Science and Technology of China, Hefei, Anhui 230036, PR China;1. Medicinal Chemistry Department, Faculty of Pharmacy, Minia University, Minia, Egypt;2. Pharmaceutical Chemistry Department, Faculty of Pharmacy, Deraya University, Minia, Egypt;3. Computational Chemistry Laboratory, Chemistry Department, Faculty of Science, Minia University, Minia, Egypt;4. Cancer Biology Laboratory, Center of Excellence for Advanced Sciences, National Research Center, Cairo, Egypt;1. Pharmaceutical Chemistry Department, Faculty of Pharmacy, Ahram Canadian University, Giza, Egypt;2. Pharmaceutical Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt;3. Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt;1. Department of Biochemistry and Molecular Biology, University of Nebraska Medical Center, Omaha, NE, USA;2. Kaohsiung Chang Gung Memorial Hospital, Kaohsiung, Taiwan, ROC;3. Department of Chemistry, Clark Atlanta University, Atlanta, GA, USA;4. Department of Biological Sciences, Clark Atlanta University, Atlanta, GA, USA;5. Center for Cancer Research and Therapeutic Development, Clark Atlanta University, Atlanta, GA, USA;6. Laboratory for Electro-Optical Materials & NASA Center for High Performance Polymers and Composites, Clark Atlanta University, Atlanta, GA, USA;7. Eppley Institute for Research in Cancer and Allied Diseases, University of Nebraska Medical Center, Omaha, NE, USA;8. Department of Surgery/Urology, University of Nebraska Medical Center, Omaha, NE, USA;9. School of Pharmacy, Kaohsiung Medical University, Kaohsiung 807, Taiwan, ROC |
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| Abstract: | A library of new imidazopyridine linked triazole hybrid conjugates (8a-r) were designed, synthesized and evaluated for their cytotoxicity against four cancer cell lines namely, human lung (A549), human prostate (DU-145), human colon (HCT-116) and breast (MDA-MB 231) cancer. These conjugates exhibited good to moderate activity against the tested human cancer cell lines. Two of the conjugates (8g and 8j) showed significant antitumor activity against human lung cancer cell line (A549) with IC50 values of 0.51 µM and 0.63 µM respectively. Flow cytometry analysis revealed that these conjugates arrested the cell cycle at G2/M phase in human lung cancer cell line (A549). Immune-histochemistry and tubulin polymerization assay suggest inhibition of tubulin. Hoechst staining, annexin V and DNA fragmentation by tunnel assay suggested that these compounds induce cell death by apoptosis. Overall, the current study demonstrates that the synthesis of imidazopyridine linked triazole conjugates as promising anticancer agents causing G2/M arrest and apoptotic-inducing ability. |
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| Keywords: | Imidazopyridine Triazoles Tubulin Apoptosis Lung cancer |
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