کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1358688 | 981357 | 2012 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis of retinoid enhancers based on 2-aminobenzothiazoles for anti-cancer therapy
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
Indole-3-amides and dipeptides were produced from 2-aminobenzothiazoles using the PyBop peptide coupling reagent. These analogues were tested in anti-cancer cell viability assays against SH-SY5Y neuroblastoma and MDA-MB-231 breast adenocarcinoma cell lines, and were found to exhibit cytotoxic activities at concentrations ranging from 0.1 to 20 μM. These compounds were also found to act additively with a low dosage of 13-cis-retinoic acid in neuroblastoma cells. Then, using neuroblastoma cells transfected to stably overexpress the RARβ2 gene, a SAR was developed for the indole-3-amides. Real-time PCR was also used to demonstrate their RARβ2 agonistic activity.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 23, 1 December 2012, Pages 6877–6884
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 23, 1 December 2012, Pages 6877–6884
نویسندگان
Christopher R. Gardner, Belamy B. Cheung, Jessica Koach, David StC. Black, Glenn M. Marshall, Naresh Kumar,