91444-18-7Relevant articles and documents
ESTROGEN RECEPTOR TARGETING ANTAGONISTS
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Paragraph 0031; 0106-0108, (2020/05/07)
The present disclosure relates to compounds that act as antagonists via binding to the ER ligand binding domain non-covalently or covalently, or act as both antagonists and ER protein degraders, and the synthesis of the same. Further, the present disclosure teaches the utilization of such compounds in a treatment for proliferative diseases, including cancer, particularly breast cancer, and especially ER+ breast cancer.
METHODS OF PREPARING BAZOEDOXIFENE
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Paragraph 0095-0100, (2018/10/16)
The present invention relates to novel bazedoxifene or to a method for producing a pharmaceutically acceptable salt thereof. The production method according to the present invention can provide the bazedoxifene with high purity and high yield, and is economical and environmentally friendly in terms of time and cost due to a relatively simple manufacturing process to be usefully applied to mass production.COPYRIGHT KIPO 2018
Synthesis, antiproliferative and pro-apoptotic activity of 2-phenylindoles
Kelly, Patrick M.,Bright, Sandra A.,Fayne, Darren,Pollock, Jade K.,Zisterer, Daniela M.,Williams, D. Clive,Meegan, Mary J.
, p. 4075 - 4099 (2016/08/23)
Breast cancer is the second most common cancer worldwide after lung cancer with the vast majority of early stage breast cancers being hormone-dependent. One of the major therapeutic advances in the clinical treatment of breast cancer has been the introduction of selective estrogen receptor modulators (SERMs). We describe the design and synthesis of novel SERM type ligands based on the 2-arylindole scaffold to selectively target the estrogen receptor in hormone dependent breast cancers. Some of these novel compounds are designed as bisindole type structures, while others are conjugated to a cytotoxic agent based on combretastatin A4 (CA4) which is a potent inhibitor of tubulin polymerisation. The indole compounds synthesised within this project such as 31 and 86 demonstrate estrogen receptor (ER) binding and strong antiproliferative activity in the ER positive MCF-7 breast cancer cell line with IC50values of 2.71?μM and 1.86?μM respectively. These active compounds induce apoptotic activity in MCF-7 cells with minimal effects on normal peripheral blood cells. Their strong anti-cancer effect is likely mediated by the presence of two ER binding ligands for 31 and an ER binding ligand combined with a cytotoxic agent for 86.