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Synthesis and Cytotoxic Evaluation of Novel 3-Substituted Derivatives of 2-Indolinone
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نویسنده
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Mokhtaria Shaya ,Mosaddegh Mahmoud ,Hamzeloo Moghadam Maryam ,Soleymani Zohreh ,Kobarfard Farzad
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منبع
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iranian journal of pharmaceutical research - 2012 - دوره : 11 - شماره : 2 - صفحه:411 -421
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چکیده
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The assessment of the degree or rate of cellular proliferation and cell viability is critical for the assessment of the effects of drugs on both normal and malignant cell populations. in the present study, a few novel 3-substituted derivatives of 2-indolinones were synthesized by condensation of substituted oxindole or isatin derivatives with appropriate aldehydes or primary aromatic amines respectively. the synthesized compounds were screened for their cytotoxicity against ht-29 (human colon adenocarcinoma cell line) and mcf-7 (human breast adenocarcinoma cell line) cells using short term cytotoxicity mtt assay protocol. a few derivatives with ic50 < 10 μm were identified among them. the compound bearing 5-bromo substitution was the most potent derivative. global physicochemical properties for compounds iva-e and va-h were calculated and the two most active compounds (iva and ivb) showed similar clog p-values
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کلیدواژه
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3- substituted derivatives of 2-indolinones; Indole derivatives; cytotoxicity; Colon and breast cancer; MTT assay
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آدرس
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shahid beheshti university of medical sciences, School of Pharmacy, Department of Medicinal Chemistry, ایران. shahid beheshti university of medical sciences, School of Pharmacy, Student Research Committee, ایران, shahid beheshti university of medical sciences, Traditional Medicine and Materia Medica Research Center, ایران, shahid beheshti university of medical sciences, Traditional Medicine and Materia Medica Research Center, ایران, shahid beheshti university of medical sciences, School of Pharmacy, Department of Medicinal Chemistry, ایران, shahid beheshti university of medical sciences, School of Pharmacy, Department of Medicinal Chemistry, ایران
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Authors
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