14982-15-1Relevant articles and documents
An efficient, practical synthesis of 2-methoxyestradiol
Xin, Minhang,You, Qidong,Xiang, Hua
, p. 53 - 56 (2010)
An efficient and practical scheme to synthesize 2-methoxyestradiol has been developed. The key step was the copper-mediated methoxylation using ethyl acetate as a co-catalyst to introduce a methoxyl group. These synthetic procedures of four steps from 17β-estradiol as starting material gave 2-methoxyestradiol with a 61% overall yield.
COMPOUNDS AND METHODS FOR TRANS-MEMBRANE DELIVERY OF MOLECULES
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Paragraph 0036, (2018/07/31)
A system for delivery of drugs, and especially genetic drugs such as siRNA or antisense oligonucleotides (ASO) across biological membranes is provided. It comprises a trans- membrane delivery moiety, energized by the membrane internal electrical field, an
PRO-DRUGS AND RELATED METHODS
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Paragraph 0048, (2017/02/24)
The invention relates to Pro-drugs, comprising red-ox-sensitive cleavage sites. The compounds may be utilized in medical practice for targeting of si RNA, antisense oligonucleotides or protein-based therapeutics to the cytoplasmatic compartment of cells both in vitro or in vivo, in a subject in need.
17β-Arylsulfonamides of 17β-aminoestra-1,3,5(10)-trien-3-ol as highly potent inhibitors of steroid sulfatase
Mostafa, Yaser A.,Taylor, Scott D.
, p. 1535 - 1544 (2012/04/23)
Steroid sulfatase (STS) catalyzes the desulfation of biologically inactive sulfated steroids to yield biologically active desulfated steroids and is currently being examined as a target for therapeutic intervention for the treatment of breast and other steroid-dependent cancers. Here we report the synthesis of a series of 17β-arylsulfonamides of 17β-aminoestra-1,3, 5(10)-trien-3-ol and their evaluation as inhibitors of STS. Some of these compounds are among the most potent reversible STS inhibitors reported to date. Introducing n-alkyl groups into the 4′-position of the 17β-benzenesulfonamide derivative resulted in an increase in potency with the n-butyl derivative exhibiting the best potency with an IC50 of 26 nM. A further increase in carbon units (to n-pentyl) resulted in a decrease in potency. Branching of the 4′-n-propyl group resulted in a decrease in potency while branching of the 4′-n-butyl group (to a tert-butyl group) resulted in a slight increase in potency (IC50= 18 nM). Studies with 3′- and 4′-substituted substituted 17β-benzenesulfonamides with small electron donating and electron withdrawing groups revealed the 3′-bromo and 3′-trifluoromethyl derivatives to be excellent inhibitors with IC50's of 30 and 23 nM, respectively. The 17β-2′-naphthalenesulfonamide was also an excellent inhibitor (IC50= 20 nM) while the 17β-4′-phenylbenzenesulfonamide derivative was the most potent inhibitor of all the compounds studied with an IC50 of 9 nM.
