Synthesis and biological evaluation of new bisindole-imidazopyridine hybrids as apoptosis inducers |
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| Affiliation: | 1. Centre for Semio Chemicals, CSIR-Indian Institute of Chemical Technology (IICT), Hyderabad 500007, India;2. Academy of Scientific and Innovative Research, New Delhi 110 025, India;3. Vaccine Immunology Laboratory, Natural Product Chemistry Division, CSIR-Indian Institute of Chemical Technology (IICT), Hyderabad 500007, India;4. Department of Chemistry, Jawaharlal Nehru Technological University, Hyderabad 500085, India;5. School of Pharmaceutical Education and Research (SPER), Jamia Hamdard, New Delhi 110062, India;1. Academy of Scientific and Innovative Research (AcSIR), New Delhi 110001, India;2. Agroprocessing and Natural Products Division, CSIR-National Institute for Interdisciplinary Science and Technology, Thiruvananthapuram 695019, Kerala, India;3. Chemical Sciences and Technology Division, CSIR-National Institute for Interdisciplinary Science and Technology, Thiruvananthapuram 695019, Kerala, India;1. Department of Chemistry, Faculty of Science, University of Jiroft, Jiroft, 7867161167, Iran;2. Department of Chemical Engineering, Faculty of Mining,Civil and Chemical Engineering, Birjand University of Technology, Birjand, 97175/569, Iran;3. Department of Chemistry, Isfahan University of Technology, Isfahan, Iran;1. Department of Applied Chemistry, Graduate School of Technology, Industrial and Social Sciences, Tokushima University, 2-1 Minamijosanjima-cho, Tokushima 770-8506, Japan;2. Institute of Post-LED Photonics, Tokushima University, 2-1 Minamijosanjima-cho, Tokushima 770-8506, Japan;3. Research Cluster on “Innovative Chemical Sensing”, Tokushima University, 2-1 Minamijosanjima-cho, Tokushima 770-8506, Japan;4. Department of Applied Chemistry and Biotechnology, Graduate School of Engineering, Chiba University, 1-33 Yayoi-cho, Inage-ku, Chiba 263-8522, Japan;1. School of Chemical Engineering, Taishan Medical University, Taian, Shandong 271016, PR China;1. Medicinal Chemistry and Pharmacology Division, CSIR-Indian Institute of Chemical Technology (IICT), Hyderabad, 500007, India;2. Academy of Scientific and Innovative Research, CSIR-Indian Institute of Chemical Technology (IICT), Hyderabad, 500007, India;3. Chemistry Department, College of Science, King Saud University, Riyadh, 11451, Saudi Arabia |
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| Abstract: | A series of diindolylmethanes (5a-t) were designed, synthesized, and examined for their cytotoxicity against four human cancer cell lines like prostate (DU-145), lung (A549), breast (MCF-7) and cervical cancer (HeLa). These results revealed that among all the hybrids, two (5k and 5r) were identified and exhibited significant cytotoxic effect against A549 cancer cells with IC50 values of 1.65 ± 0.3 and 1.80 ± 0.8 µM respectively. To investigate the reasons for the cytotoxic activity, the conventional biological assays were carried out with 5k and 5r on the A549 cancer cells. Both hybrids led to the arrest of A549 cell lines at the G2/M phase of the cell cycle and strongly induced apoptosis. Further the apoptotic effects of 5k and 5r were confirmed by ROS, annexin-V FITC, and mitochondrial membrane potential. Moreover, structure–activity relationships were elucidated with various substitutions on these hybrids. |
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| Keywords: | Bisindole-imidazopyridine Heterocyclic ROS Cytotoxicity Apoptosis |
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