【摘 要】
：
Tamoxifen remains the first line therapy for estrogen receptor positive (ER+) breast cancer.However, polymorphisms of the gene encoding P450 2D6 could result in no protein expression or no CYP2D6 enzy
【机 构】
：
Xavier University of Louisiana USA
【出 处】
：
2013第三届内分泌与代谢大会暨2013第二届糖尿病大会
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Tamoxifen remains the first line therapy for estrogen receptor positive (ER+) breast cancer.However, polymorphisms of the gene encoding P450 2D6 could result in no protein expression or no CYP2D6 enzymatic activity, and may significantly reduce the benefit of the hormone therapy.Additionally, persistent and widespread side effects such as hot flash from tamoxifen treatment often lead to patient non-compliance and seriously affect post-surgery quality of life, particularly in premenopausal women.To address these clinical problems we designed and synthesized three 4-hydroxytamoxifen bioisosteres utilizing a boron-aryl carbon bond that can be oxidized under physiological conditions to yield 4-hydroxytamoxifen.
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