135857-20-4Relevant articles and documents
A process for the preparation of intermediates palestinian multi-past fragrance acetate
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Paragraph 0089-0093, (2017/01/31)
The invention discloses a method for preparing a bazedoxifene acetate intermediate. The preparation method comprises the following steps: 1, condensing 4-hydroxybenzaldehyde S01 and alkylate S02 to prepare a 4-formyl phenoxy derivative M01; 2, performing
Synthesis and biological evaluation of 2-Phenoxyacetamide analogues, a novel class of potent and selective monoamine oxidase inhibitors
Shen, Wei,Yu, Shian,Zhang, Jiaming,Jia, Weizheng,Zhu, Qing
, p. 18620 - 18631 (2015/01/08)
Monoamine oxidases (EC 1.4.3.4; MAOs), a family of FAD-containing enzymes, is an important target for antidepressant drugs. In this paper, a series of 2-phenoxyacetamide analogues were synthesized, and their inhibitory potency towards monoamine oxidases A (MAO-A) and B (MAO-B) were evaluated using enzyme and cancer cell lysate. 2-(4-Methoxyphenoxy)acetamide (compound 12) (SI = 245) and (2-(4-((prop-2- ynylimino)methyl)phenoxy)acetamide (compound 21) (IC50MAO-A = 0.018 μM, IC50MAO-B = 0.07 μM) were successfully identified as the most specific MAO-A inhibitor, and the most potent MAO-A/-B inhibitor, respectively. The inhibitory activities of these two compounds in living cells were also further evaluated utilizing HepG2 and SHSY-5Y cell lysates.
Inhibition of γ-secretase by the CK1 inhibitor IC261 does not depend on CK1δ
H?ttecke, Nicole,Liebeck, Miriam,Baumann, Karlheinz,Schubenel, Robert,Winkler, Edith,Steiner, Harald,Schmidt, Boris
supporting information; experimental part, p. 2958 - 2963 (2010/08/19)
CK1 and γ-secretase are interesting targets for therapeutic intervention in the treatment of cancer and Alzheimer's disease. The CK1 inhibitor IC261 was reported to inhibit γ-secretase activity. The question is: Does CK1 inhibition directly influence γ-se