Design and synthesis of new benzoxazole/benzothiazole-phthalimide hybrids as antitumor-apoptotic agents |
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| Institution: | 1. Department of Chemistry, Jamia Millia Islamia, New Delhi, 110025, India;2. Department of Chemistry, Aligarh Muslim University, Aligarh, 202002, India;3. Department of Biosciences, Jamia Millia Islamia, New Delhi, 110025, India;1. Departamento de Ciências Farmacêuticas, Centro de Ciências da Saúde, Universidade Federal de Pernambuco, 50740-520, Recife, PE, Brazil;2. Departamento de Biofísica e Fisiologia, Programa de Pós-Graduação em Ciências Farmacêuticas, Universidade Federal do Piauí, 64049-550, Teresina, PI, Brazil;3. Departamento de Fisiologia e Farmacologia, Faculdade de Medicina, Universidade Federal do Ceará, 60430-270, Fortaleza, CE, Brazil;4. Fundação Oswaldo Cruz, 60180-900, Fortaleza, CE, Brasil;5. Departamento de Física e Informática, Instituto de Física, Universidade de São Paulo, 13560-970, São Carlos, SP, Brazil;6. Departamento de Ciências da Vida, Universidade do Estado da Bahia, 41150-000, Salvador, BA, Brazil;7. Hospital São Rafael, 41253-190, Salvador, BA, Brazil;1. Department of Medicinal Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt;2. Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt;1. Pharmaceutical Chemistry Department, College of Pharmacy, Jouf University, Aljouf 2014, Saudi Arabia;2. Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Beni-Suef University, Beni-Suef 62514, Egypt;3. School of Pharmaceutical Sciences, University Sains Malaysia, 11800 Pulau Pinang, Malaysia;1. Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry Education and Yunnan Province, School of Chemical Science and Technology, Yunnan University, Kunming, 650091, PR China;2. Laboratory of Molecular Genetics of Aging and Tumor, Medical School, Kunming University of Science and Technology, Kunming, 650500, PR China;3. Biomedical Department, Yunnan Cancer Hospital, The Third Affiliated Hospital of Kunming Medical University, Kunming, 650118, PR China;4. Institute of Drug Research and Development, Kunming Pharmaceutical Corporation, Kunming, 650100, PR China;5. Department of Anorectal, Kunming Municipal Hospital of Traditional Chinese Medicine, Kunming, 650011, PR China;6. School of Clinical Medicine, Dehong Vocational College, Mangshi, 678400, China;1. Academy of Scientific and Innovative Research (AcSIR), CSIR-Human Resource Development Centre (CSIR-HRDC) Campus, Ghaziabad, 201 002, Uttar Pradesh, India;2. Department of Organic Synthesis & Process Chemistry, CSIR-Indian Institute of Chemical Technology (IICT), Hyderabad, 500 007, India;3. Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Hyderabad, 500 037, India;4. Centre for Advanced Materials & Industrial Chemistry (CAMIC), School of Science, RMIT University, GPO Box 2476, Melbourne, 3001, Australia;5. Phenomics Laboratory, School of Science, RMIT University, Plenty Road, PO Box 71, Bundoora, Victoria, 3083, Australia;6. Department of Chemistry, Keshav Memorial Institute of Commerce and Sciences, Narayanguda, Hyderabad, 500 029, India;7. School of Pharmaceutical Education and Research (SPER), Jamia Hamdard, New Delhi, 110 062, India |
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| Abstract: | Herein, we synthesized a series of twelve benzoxazole and benzothiazole derivatives incorporated with phthalimide core as anticancer agents. The most active compounds were 5a and 5g against HepG2 and MCF7 cell lines with IC50 = 0.011 and 0.006 μM, respectively.They evaluated against EGFR and HER2 enzymes. From cell cycle analysis, it was observed that test compounds exerted pre G1 apoptosis and cell cycle arrest at G2/M phase. The achieved results suggested that apoptosis was due to activation of caspase-7 and caspase-9. EGFR was chosen as a biological target for carrying molecular modeling study for the newly synthesized compounds. |
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| Keywords: | Benzothiazole Benzoxazole Phthalimide Antitumor Synthesis |
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