Multistep synthesis and screening of heterocyclic tetrads containing furan,pyrazoline, thiazole and triazole (or oxadiazole) as antimicrobial and anticancer agents |
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| Institution: | 1. Department of Pharmaceutical Sciences, College of Pharmacy & Health Sciences, Ajman University, Ajman, PO Box 346, United Arab Emirates;2. Center of Medical and Bio-allied Health Sciences Research, Ajman University, Ajman, United Arab Emirates;3. Rallis India Limited, A TATA Enterprise, # 73/1, 1C, 1D, Byregowda Industrial Layout, Srigandhanagara, Hegganahalli, Peenya, Bangalore 560091, Karnataka, India;4. East West College of Pharmacy, #63, I Phase, BEL Layout, Bharathnagar, Vishwaneedam PO, Bangalore 560091, Karnataka, India;5. Department of Pharmaceutical Sciences, Vignan''s Foundation for Science, Technology and Research, Guntur, Andhra Pradesh, India;6. Department of Pharmaceutical Chemistry, Vignan Pharmacy College, Jawaharlal Nehru Technological University, Vadlamudi 522213, Andhra Pradesh, India;7. Faculty of Pharmaceutical Sciences, Shri Shankaracharya Technical Campus, Junwani, Bhilai 491001, Chhattisgarh, India;8. Department of Chemistry, M.S. Ramaiah Institute of Technology (Affiliated to Visvesvaraya Technological University, Belgaum), Bengaluru, Karnataka, India;9. Department of Pharmaceutical Medicinal Chemistry, Faculty of Pharmacy, Horus University-Egypt, New Damietta 34518, Egypt |
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| Abstract: | In the present study novel heterocyclic tetrads containing furan, pyrazoline, thiazole and triazole (or oxadiazole) (1, 2, 3, 4a-e and 5a-e) were designed and synthesized and investigated for their antimicrobial (against selected bacteria and fungi) and anticancer potential. The molecules 4e and 5e containing 4-fluoro phenyl and 4-fluoro benzyl substituents showed promising antimicrobial (antibacterial and antifungal activities with MICs ranging between 0.5 and 8 µg/mL. Compounds 3 exhibited potent anticancer activity with an IC50 value of 0.49 ± 1.45 µM against the human gastric cancer cell line (BGC-823) whereas compound 4e displayed an IC50 value of 0.65 ± 0.53 µM against breast cancer (MCF-7) cell line respectively. All compounds showed selective toxicity against the cancer cell lines compared to human normal liver cell lines. Molecular docking studies of the most potent compounds (3 and 4e) against selected microbial and cancer proteins revealed the crucial binding interactions of the potent compounds with the target enzymes. Compounds 3 and 4e are promising lead molecules to be developed as potential drug candidates. |
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| Keywords: | Heterocyclic tetrads Cancer Microbial infections Docking |
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