کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10584142 | 981326 | 2013 | 19 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Multidimensional optimization of promising antitumor xanthone derivatives
ترجمه فارسی عنوان
بهینه سازی چند بعدی از امیدوارکننده های مشتقات زانتونوئید ضد تومور
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
چکیده انگلیسی
A promising antitumor xanthone derivative was optimized following a multidimensional approach that involved the synthesis of 17 analogues, the study of their lipophilicity and solubility, and the evaluation of their growth inhibitory activity on four human tumor cell lines. A new synthetic route for the hit xanthone derivative was also developed and applied for the synthesis of its analogues. Among the used cell lines, the HL-60 showed to be in general more sensitive to the compounds tested, with the most potent compound having a GI50 of 5.1 μM, lower than the hit compound. Lipophilicity was evaluated by the partition coefficient (Kp) of a solute between buffer and two membrane models, namely liposomes and micelles. The compounds showed a log Kp between 3 and 5 and the two membrane models showed a good correlation (r2 = 0.916) between each other. Studies concerning relationship between solubility and structure were developed for the hit compound and 5 of its analogues.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 21, Issue 11, 1 June 2013, Pages 2941-2959
Journal: Bioorganic & Medicinal Chemistry - Volume 21, Issue 11, 1 June 2013, Pages 2941-2959
نویسندگان
Carlos M.G. Azevedo, Carlos M.M. Afonso, Diana Sousa, Raquel T. Lima, M. Helena Vasconcelos, Madalena Pedro, João Barbosa, Arlene G. Corrêa, Salette Reis, Madalena M.M. Pinto,