New azafluorenones with cytotoxic and carbonic anhydrase inhibitory properties: 2-Aryl-4-(4-hydroxyphenyl)-5H-indeno[1,2-b]pyridin-5-ones |
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| Institution: | 1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ataturk University, Erzurum, Turkey;2. Division of Pharmacology, Meikai University School of Dentistry, Sakado, Saitama, Japan;3. Department of Chemistry, Faculty of Science, Ataturk University, Erzurum, Turkey;4. Neurofarba Department, Sezione di Scienza Farmaceutiche e Nutraceutiche, Universita egli Studi di Firenze, Via U. Schiff 6, 50019 Sesto Fiorentino (Florence), Italy;1. Panjwani Center for Molecular Medicine and Drug Research, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270 Pakistan;2. HEJ Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270 Pakistan;1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, 26470 Eski?ehir, Turkey;2. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Bülent Ecevit University, Zonguldak, Turkey;3. Department of Nano-Science and Nano-Engineering, Faculty of Engineering, Atatürk University, 25240 Erzurum, Turkey;4. Department of Food Technology, Erzurum Vocational Training School, Atatürk University, 25240 Erzurum, Turkey;1. Department of Chemistry, University of Delhi, Delhi 110007, India;2. Dyal Singh College, University of Delhi, Lodhi Road, Delhi 110003, India;1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ataturk University, Erzurum 25240, Turkey;2. Meikai University Research Institute of Odontology (M-RIO), Sakado, Saitama 350-0283, Japan;3. Neurofarba Department, Sezione di Scienza Farmaceutiche e Nutraceutiche, Universita degli Studi di Firenze, Via U. Schiff 6, 50019 Sesto Fiorentino (Florence), Italy;4. Latvian Biomedical Research and Study Center, Ratsupites 1, Riga, Latvia;5. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Agri Ibrahim Cecen University, Agri 04100, Turkey;1. Department of Chemistry, Kurukshetra University, Kurukshetra 136119, Haryana, India;2. Department of Chemistry, National Institute of Technology Kurukshetra, Kurukshetra 136119, Haryana, India;3. Ch. Mani Ram Godara Government College for Women, Bhodia Khera, Fatehabad 125050, Haryana, India;4. Department of Neurosciences, Psychology, Drug Research and Child Health, Pharmaceutical and Nutraceutical Section, University of Florence, Florence, Italy |
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| Abstract: | New azafluorenones, 2-aryl-4-(4-hydroxyphenyl)-5H-indeno1,2-b]pyridin-5-ones, were prepared to evaluate their cytotoxic/anticancer properties, also their inhibitory effects on hCA I and II isoenzymes. Aryl part was changed as phenyl (H1), 4-methylphenyl (H2), 4-methoxyphenyl (H3), 4-fluorophenyl (H4), 4-bromophenyl (H5), 4-chlorophenyl (H6), 3-hydroxyphenyl (H7), and 4-hydroxyphenyl (H8)]. The structure of the synthesized compounds was characterized by 1H NMR, 13C NMR and HRMS spectra.Cytotoxicity results of the series pointed out that the compounds H6 (PSE: 28.0) and H5 (PSE: 27.3), with the highest potency selectivity expression (PSE) value, can be considered as leader compounds of the study in designing novel anticancer agents. Additionally, all azafluorenones synthesized showed a good inhibition profile towards hCA I and II isoenzymes in the range of 54.14–73.72 nM and 67.28–76.15 nM, respectively.The compounds H5 and H6 can be considered for further designs with their cytotoxic and CA inhibitory profiles. |
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| Keywords: | Azafluorenone Phenol Cytotoxicity Carbonic anhydrase |
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