کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1371409 | 981845 | 2011 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Novel second generation analogs of eribulin. Part II: Orally available and active against resistant tumors in vivo
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Novel second generation analogs of eribulin. Part II: Orally available and active against resistant tumors in vivo Novel second generation analogs of eribulin. Part II: Orally available and active against resistant tumors in vivo](/preview/png/1371409.png)
چکیده انگلیسی
Eribulin mesylate is a newly approved treatment for locally advanced and metastatic breast cancer. We targeted oral bioavailability and efficacy against multidrug resistant (MDR) tumors for further work. The design, synthesis and evaluation of novel amine-containing analogs of eribulin mesylate are described in this part. Attenuation of basicity of the amino group(s) in the C32 side-chain region led to compounds with low susceptibility to PgP-mediated drug efflux. These compounds were active against MDR tumor cell lines in vitro and in xenograft models in vivo, in addition to being orally bioavailable.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 6, 15 March 2011, Pages 1634–1638
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 6, 15 March 2011, Pages 1634–1638
نویسندگان
Sridhar Narayan, Eric M. Carlson, Hongsheng Cheng, Krista Condon, Hong Du, Sean Eckley, Yongbo Hu, Yimin Jiang, Vipul Kumar, Bryan M. Lewis, Philip Saxton, Edgar Schuck, Boris M. Seletsky, Karen Tendyke, Huiming Zhang, Wanjun Zheng, Bruce A. Littlefield,