synthesis and cytotoxic activity of novel 9-[hydroxy(substitutedphenyl) methyl]-2,2-dimethyl-2,3,8,9-tetrahydro-4h,10h-pyrano [2,3-f ]chromene-4,10-diones
نویسندگان
چکیده
chromanone derivatives demonstrate remarkable cytotoxity against a varieties of cancer cell lines. novel 9-[hydroxy(substitutedphenyl)methyl]-2,2-dimethyl-2,3,8,9- tetrahydro-4h,10h-pyrano[2,3-f]chromene-4,10-diones as glyasperin analogues were synthesized in four steps from known 4-chromone 1. the key step was the preparation of chromane dione 5a by regioselective intramolecular cyclization reaction in 85% yield. condensation of 5a with substituted aromatic aldehydes afforded corresponding alpha hydroxybenzyl analogues 6a-6e. the cytotoxic study of the synthesized compounds against breast cancer human cell line (t47d) showed moderate cytotoxic activities (ic50=16-40 μm) compared to the positive control drug vincristin (ic50=2.5 μm).
منابع مشابه
Synthesis and Cytotoxic Activity of Novel 9-[Hydroxy(Substitutedphenyl) Methyl]-2,2-Dimethyl-2,3,8,9-Tetrahydro-4H,10H-Pyrano [2,3-f ]Chromene-4,10-Diones
Chromanone derivatives demonstrate remarkable cytotoxity against a varieties of cancer cell lines. Novel 9-[hydroxy(substitutedphenyl)methyl]-2,2-dimethyl-2,3,8,9- tetrahydro-4H,10H-pyrano[2,3-f]chromene-4,10-diones as Glyasperin analogues were synthesized in four steps from known 4-chromone 1. The key step was the preparation of chromane dione 5a by regioselective intramolecular c...
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Drug Design and Development Research Center, Tehran University of Medicinal Sciences, Tehran, Iran Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medicinal Sciences, Tehran, Iran Medicinal and Natural Product Chemistry Research Center, Shiraz University of Medical Sciences, Shiraz, Iran *E-mail: [email protected] Received December 9, 2012 DOI 10.1002/jh...
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there has been special interest in the chemistry of quinolone and pyrimidine derivatives due to their diverse biological activities such as anticonvulsant, anti-malarial agents, antibacterial, antiviral, cytostatic, antithelemintic, antigenotoxic, anti-cancer agents. these compounds are also used as targeting delayed-type hypersensivity and anti-convulsant agents. as a part of our research work...
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عنوان ژورنال:
iranian journal of chemistry and chemical engineering (ijcce)ناشر: iranian institute of research and development in chemical industries (irdci)-acecr
ISSN 1021-9986
دوره 29
شماره 4 2010
کلمات کلیدی
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