2352-19-4Relevant articles and documents
ANTI-CANCER NUCLEAR HORMONE RECEPTOR-TARGETING COMPOUNDS
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Page/Page column 142, (2020/11/30)
The disclosure relates to anti-cancer compounds derived from nuclear steroid receptor binders, to products containing the same, as well as to methods of their use and preparation.
Stereoselective synthesis of some methyl-substituted steroid hormones and their in vitro cytotoxic activity against human gastric cancer cell line MGC-803
Li, Chun,Qiu, Wenwei,Yang, Zhengfeng,Luo, Jian,Yang, Fan,Liu, Mingyao,Xie, Juan,Tang, Jie
experimental part, p. 859 - 869 (2010/10/18)
A series of 3-, 7-, 15-, and 16-methyl-substituted steroid analogs were synthesized via a highly stereoselective 1,6-conjugate addition. Under the catalysis of CuBr, AlMe3 reacted with four steroid dienone precursors to afford either the corresponding α-epimer of C-3 and C-7 methyl-substituted steroids as the major products, and the ratio of α/β was up to 10/1. No β-epimer has been detected for methyl addition at C-16. However, under the same reaction conditions, enantioselective methyl addition at C-15 afforded the 15β-epimer as the major product. The preliminary SAR analysis showed that the methyl substituents at C-7α and C-15β positions lead to a dramatical increase in potency against human gastric cancer cell line MGC-803.
Functionalization of testosterone at position 7 and synthesis of 7-(3-methoxypropyl)-4-androsten-17-ol-3-one
Bastien, Dominic,Nault, Josee,Berube, Gervais
experimental part, p. 1884 - 1892 (2009/11/30)
An efficient transformation of the terminal alkene function of 7-allyltestosterone is reported along with the stereospecific synthesis of 7-(3-methoxypropyl)-4-androsten-17-ol-3-one.
