کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10583900 | 981312 | 2013 | 11 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and anti-tumor activity of carbohydrate analogues of the tetrahydrofuran containing acetogenins
ترجمه فارسی عنوان
سنتز و فعالیت ضد تومور از آنالوگهای کربوهیدرات استاتوژنین حاوی تتراهیدروفوران
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
چکیده انگلیسی
The tetrahydrofuran (THF) containing annonaceous acetogenins (AAs) are attractive candidates for drug development because of their potent cytotoxicity against a wide range of tumors and their relatively simple and robust structures. Replacement of the THF segment with a sugar residue may deliver analogues with improved tumor selectivity and pharmacokinetics and are therefore attractive for drug development. As a first test to the feasibility of such structures, a set of such monosaccharide analogues was synthesized and assayed against four human tumor cell lines, cervical (HeLa), breast (MDA-MB231), T-cell leukemia (Jurkat) and prostate (PC-3). Certain analogues showed low micromolar activity that was comparable to a structurally similar, naturally occurring mono-THF acetogenin. A preliminary examination of the structure-activity profile of these carbohydrate analogues suggests that they have a similar mechanism of action as their THF congeners.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 21, Issue 21, 1 November 2013, Pages 6554-6564
Journal: Bioorganic & Medicinal Chemistry - Volume 21, Issue 21, 1 November 2013, Pages 6554-6564
نویسندگان
Stewart Bachan, K.A. Tony, Akira Kawamura, Diego Montenegro, Anjali Joshi, Himanshu Garg, David R. Mootoo,