کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
10593291 981806 2013 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
New cytotoxic benzosuberene analogs. Synthesis, molecular modeling and biological evaluation
ترجمه فارسی عنوان
آنالوگهای جدید بنوسوبرن سیتوتوکسیک. سنتز، مدل سازی مولکولی و ارزیابی بیولوژیکی
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
چکیده انگلیسی
In this Letter we describe the synthesis and biological evaluation of new benzosuberene analogs with structural modifications on the B-ring. The focus was initially to probe the chemical space around the B-ring C-8 position. This position was readily available for derivatization chemistry using our recently developed new synthesis for this compound class. Furthermore, we describe two new B-ring analogs, one containing a diene and the other a cyclic ether group. Both new analogs show excellent potencies in tumor cell proliferation assays. In addition, we describe molecular modeling studies that provide a binding rationale for reference compound 8 in the colchicine binding site using the known colchicine crystal structure. We also examine whether the cell based potency data obtained with selected new analogs are supported by modeling results.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 23, Issue 24, 15 December 2013, Pages 6688-6694
نویسندگان
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