期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 52, 期 -, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2021.128383
关键词
Selective estrogen receptor modulators; Tamoxifen; Raloxifene; Breast cancer; Estrogen receptor alpha
资金
- Reed College Science Research Fellowship
- Reed College
- Marshall W. Cronyn Fellowship
The report highlights the potential of Selective Estrogen Receptor Modulators (SERMs) in breast cancer treatment, presenting an unexplored tamoxifen substitution pattern with favorable pharmacodynamics mimicking raloxifene.
The repurposing of old drugs for new treatments has recently garnered increased attention in the face of new diseases and declining productivity of the pharmaceutial industry. This report draws attention to potential op-portunities hiding in plain sight within the SAR of off-patent drugs. Herein we explore the untapped potential of Selective Estrogen Receptor Modulators (SERMs). SERMs are a class of molecules that have been highly influ-ential in the treatment of estrogen receptor-positive breast cancers. However, the most commonly prescribed SERM, tamoxifen, has been found to increase the risk of endometrial cancer. Another SERM, raloxifene, does not increase incidence of endometrial cancer, but has been abandoned as a breast cancer treatment. We report the design, synthesis, and evaluation of an unexplored tamoxifen substitution pattern which mimics the geometry of raloxifene to confer its favorable pharmacodynamics. This substitution pattern was found to maintain excellent binding affinity to estrogen receptor-alpha.
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