55934-10-6Relevant academic research and scientific papers
Lewis acid-mediated generation of bicyclo[5.3.0]decanes and bicyclo[4.3.0]nonanes
Deak, Holly L.,Williams, Michael J.,Snapper, Marc L.
, p. 5785 - 5788 (2005)
(Chemical Equation Presented) Fragmentation of the cyclobutane-containing adducts generated from intramolecular cycloadditions of cyclobutadiene with olefins provides rapid entry into bicyclo[5.3.0]decane and bicyclo[4.3.0]nonane ring systems. Whereas ear
Anionic Oxy-Claisen Rearrangement of a Tricyclic α-Allyloxy Ketone
Kirchner, James J.,Pratt, Daniel V.,Hopkins, Paul B.
, p. 4229 - 4232 (1988)
Preparatively useful reaction conditions for the anionic oxy-Claisen rearrangement of an α-allyloxy ketone (6) possessing acidic α- and α'-hydrogens are described.The reaction rate and efficiency are strongly influenced by both solvent and counterion.The
Synthesis, biological evaluation and molecular docking studies of indeno [1, 2-c] pyrazol derivatives as inhibitors of mitochondrial malate dehydrogenase 2 (MDH2)
Ahmadi, Farzaneh,Engel, Matthias,Baradarani, Mehdi M.
, (2021/03/15)
Hypoxia inducible factor-1 (HIF-1) is a pivotal transcription factor, which is strongly correlated with the induction of angiogenesis, tumor survival, metastasis, and cell proliferation, making it a pivotal therapeutic target for solid tumor therapeutic agents. Herein, a new series of multi-functional chemical probes were designed including principal groups, viz. adamantyl and indene, at various locations of the parent compound LW6. Molecular docking studies were performed on the designed compounds and their relationship with HIF-1α and malate dehydrogenase 2 (MDH2). Inhibition of MDH2 by our compounds was expected to decrease the NADH level. Indeed, treatment of the breast cancer cell line 4T1 led to a strong reduction of the NADH concentration. The greatest reduction in NADH production in mitochondria was observed with (E)-3-(4-((3r, 5r, 7r)-adamantan-1-yl) phenoxy)-N-(5-(piperidine-1-carbonyl)-1, 4-dihydroindeno [1, 2-c] pyrazol-3-yl) acrylamide (18: IC50 = 59 nM), and has the best inhibitory potential under hypoxic conditions (MCF-7: IC50 = 57 nM). This compound also gave one of the highest docking “higher than the score obtained with LW6 in parallel (?31.63 kcal/mol) in the initial docking runs (PDB Code: 4WLO). Other related compounds with good yields were also synthesized from docking results, and all the synthesized compounds (14, 18, 22, 26, 29, 30) were evaluated in vitro on human adenocarcinoma cell lines.
New preparation method of 4-aminoindan compound
-
, (2019/10/01)
The invention relates to a new preparation method of a 4-aminoindan compound. 4-Aminoindan is an important medical intermediate. With carboxybenzaldehyde as an initial raw material, through esterification, condensation, cyclization, reduction elimination, Curtius rearrangement, an amidogen deprotection reaction and a hydrogenation reaction in sequence, the 4-aminoindan is prepared. According to the method, the problems of difficult generation of isomers, difficult separation of substitution products and the like in a traditional method are solved, the whole preparation method is convenient toimplement, the yield is high, and the method has great industrial prospects.
METHODS USING HDAC11 INHIBITORS
-
Paragraph 0701-0702, (2018/05/16)
The present invention provides methods and uses of inhibitors of histone deacetylase 11 (HDAC11) in the treatment of diseases and/or disorders, such as, for example, cell proliferative diseases.
SUBSTITUTED BICYCLIC COMPOUNDS AS INHIBITORS OF EZH2
-
Page/Page column 123, (2014/10/15)
The present invention provides compounds of formula 1, isotopic forms, stereoisomers or tautomers thereof, or pharmaceutically acceptable salts, solvates, N-oxides, S-oxides and polymorphs thereof, and processes for their preparation. The invention further relates to pharmaceutical compositions containing said compounds and their use in the treatment of diseases or disorders mediated by EZH2 (enhancer of zeste homolog 2), particularly cancer.
AMINO-PYRIDINE-CONTAINING SPLEEN TYROSINE KINASE (SYK) INHIBITORS
-
Page/Page column 54, (2012/11/14)
The invention provides certain amino-pyridine-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and n are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
