کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1359541 | 981406 | 2014 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design, synthesis and biological evaluation of β-boswellic acid based HDAC inhibitors as inducers of cancer cell death
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
The synthesis and bio-evaluation of naturally occurring boswellic acids (BAs) as an alternate CAP for the design of new HDAC inhibitors is described. All the compounds were screened against a panel of human cancer cell lines to identify leads, which were subsequently examined for their potential to inhibit HDACs. The identified lead compound showed IC50 value of 6 μm for HDACs, found to induce G1 cell cycle arrest at significantly low concentration (1 μM) and caused significant loss in mitochondrial membrane potential at 5 and 10 μM. Furthermore, specific interactions of the lead molecule inside the catalytic domain were also studied through in silico molecular modeling.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 19, 1 October 2014, Pages 4729–4734
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 19, 1 October 2014, Pages 4729–4734
نویسندگان
Simmi Sharma, Mudassier Ahmad, Javeed Ahmad Bhat, Arvind Kumar, Manjeet Kumar, Mohmmad Afzal Zargar, Abid Hamid, Bhahwal Ali Shah,