کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1368574 981704 2016 4 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis, biological evaluation and molecular docking studies of 2-amino-3,4,5-trimethoxyaroylindole derivatives as novel anticancer agents
ترجمه فارسی عنوان
سنتز، ارزیابی بیولوژیکی و مطالعه تکینگی مولکولی مشتقات 2-amino-3،4،5-trimethoxyaroylindole به عنوان عوامل ضد سرطان جدید
کلمات کلیدی
2-آمینو-3،4،5-trimethoxyaroylindole؛ Combretastatin A-4؛ سنتز؛ ضد سرطان
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
چکیده انگلیسی

A series of novel 2-amino-3,4,5 trimethoxyaroylindole derivatives was synthesized and evaluated against selected human cancer cell lines of breast (MCF-7) and colon (HT-29). Introduction of an amino group at the C-2 position on ring A of 3,4,5-trimethoxyaroylindole derivatives resulted in novel compounds, i.e., 2-amino-3,4,5-trimethoxyaroylindole derivatives exhibiting excellent cytotoxic activity against human cancer cell lines. Substitution with methoxy group at R6 in 2-amino-3,4,5-trimethoxyaroylindole 5d exhibited excellent cytotoxic activity against MCF-7 (0.013 μM) and colon HT-29 (0.143 μM) indicating slightly higher potency than Combretastatin A-4. Molecular modeling studies of 2-amino-3,4,5-trimethoxyaroylindole derivatives have similar structural alignment as colchicine in protein (PDB code: 1SA0) and exhibited hydrogen bond interaction between para position of 3,4,5-trimethoxyphenyl ring with CYS 241 and N–H molecule of indole ring with Val 315 of receptor molecule.

A series of novel 2-amino-3,4,5 trimethoxyaroylindole derivatives was synthesized and exhibited excellent cytotoxic activity against MCF-7 (0.013 μM) and colon HT-29 (0.143 μM) indicating slightly higher potency than Combretastatin A-4. Molecular docking studies supported the promising results of anticancer activity with favorable ligand receptor interactions.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 26, Issue 9, 1 May 2016, Pages 2115–2118
نویسندگان
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