Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1371409 | Bioorganic & Medicinal Chemistry Letters | 2011 | 5 Pages |
Abstract
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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Organic Chemistry
Authors
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,