836-58-8Relevant articles and documents
N2-substituted alkoxy aromatic cyclo-2-aminopyrimidine derivative and application thereof
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Paragraph 0055-0056; 0077-0078, (2020/09/20)
The invention provides an N2-substituted alkoxy aromatic cyclo-2-aminopyrimidine derivative and application thereof. The N2-substituted alkoxy aromatic cyclo-2-aminopyrimidine derivative comprises anoptical isomer and pharmaceutically acceptable salt thereof. Preliminary pharmacodynamic indication shows that the compound disclosed by the invention has FLT3 inhibitory activity, wherein the proliferation inhibition activity is realized on various leukemia cell strains; moreover, the derivative is effective for multiple mutations of AML, such as internal tandem repeat mutation of a near-membranestructural domain and D835 point mutation of an activated ring in a kinase structural domain and almost has no inhibition effect on c-KIT. The derivative can overcome drug resistance brought by clinical point mutation, can reduce toxic and side effects of bone marrow inhibition, and can be applied to preparation of antitumor drugs. The general structural formula of the derivative is shown in thespecification.
Synthesis of tetracyclic heterocompounds as selective estrogen receptor modulators. Part 2. Process improvement for scale-up of 2,5,8-substituted 11,12-dihydro-5H-6,13-dioxabenzo[3,4]cyclohepta-[1,2-a]naphthalene derivatives
Li, Xun,Reuman, Michael,Russell, Ronald K.,Youells, Scott,Beish, Sandra,Hu, Zhiyong,Branum, Shawn,Jain, Nareshkumar,Sui, Zhihua
, p. 731 - 738 (2012/12/29)
An improved, reproducible nonchromatographic process for scale-up synthesis of 2,5,8-substituted 11,12-dihydro-5H-6,13-dioxabenzo[3,4]cyclohepta[1,2-a] naphthalene derivatives as selective estrogen receptor modulators (SERMs) is described. The titled comp
Differential response of estrogen receptor subtypes to 1,3-diarylindene and 2,3-diarylindene ligands
Clegg, Nicola J.,Paruthiyil, Sreenivasan,Leitman, Dale C.,Scanlan, Thomas S.
, p. 5989 - 6003 (2007/10/03)
Estrogen receptors (ERs) control transcription of genes important for normal human development and reproduction. The signaling networks are complex, and there is a need for a molecular level understanding of the roles of receptor subtypes ERα and ERβ in normal physiology and as therapeutic targets. We synthesized two series of ER ligands, based on a common indene scaffold, in an attempt to develop compounds that can selectively modulate ER-mediated transcription. The 3-ethyl-1,2-diarylindenes, utilizing an amide linker for the 1-aryl extension, bind weakly to the ERs. The 2,3-diarylindenes bind with high affinity to the ER subtypes and demonstrate a range of different biological activities, both in transcriptional reporter gene assays and inhibition of estradiol-stimulated proliferation of MCF-7 cells. Several ligands differentiate between ERα and ERβ subtypes at an estrogen response element (ERE), displaying various levels of partial to full agonist activity at ERα, while antagonizing estradiol action at ERβ.