791-69-5Relevant articles and documents
Prodigiosenes conjugated to tamoxifen and estradiol
Marchal, Estelle,Figliola, Carlotta,Thompson, Alison
, p. 5410 - 5427 (2017)
We report the synthesis of the first click-appended prodigiosene conjugates. Four prodigiosene conjugates of estradiol functionalised at the 7α-position were prepared, as were three prodigiosene conjugates of tamoxifen. The coupling between a prodigiosene and an 11-hydroxy estradiol derivative via an ether linkage was investigated, as was the 11- and 7-functionalisation of the estradiol core. The robustness of estradiol protecting groups was severely challenged by reactions typically used to equip such frameworks for 11- and 7-functionalisation. Specifically, and important to synthesis involving estradiol, TBS, TMS and THP are not useful protecting groups for the functionalisation of this core. When the chemical features of the therapeutic agent limit the choice of protecting group (in this case, prodigiosenes bearing aryl, NH, alkenyl and ester groups), click chemistry becomes an attractive synthetic strategy. The anti-cancer activity of the seven click prodigiosene conjugates was evaluated.
Compound for targeted ubiquitination degradation of ERalpha protein and application thereof
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, (2020/12/30)
The invention provides a compound with estrogen receptor alpha (ERalpha) activity, and particularly provides a 1,3,5-triazine compound with a general formula (I) or a general formula (II) or a pharmaceutically acceptable salt thereof. The definitions of the groups are as described in the specification. The compound disclosed by the invention has ERalpha degradation activity and can be used for preparing medicines for treating human breast cancer and endometrial cancer.
Novel steroid selective estrogen receptor modulator as well as preparation method and pharmaceutical application thereof
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Paragraph 0036; 0037; 0038, (2017/01/26)
The invention relates to the field of pharmaceutical chemistry, and discloses a novel steroid selective estrogen receptor modulator as well as a preparation method and a pharmaceutical application thereof, in particular to steroid derivatives of a general formula (I), a preparation method thereof, pharmaceutical compositions containing the compounds and a pharmaceutical application thereof. The steroid derivatives can be applicable to treat a plurality of medical indications related to postmenopausal symptoms, in particular to treat ER-(+) type breast cancer. Meanwhile, the compounds can be used to prepare medicaments as angiogenesis inhibitors. The general formula (I) is shown in the description.
