7529-87-5Relevant academic research and scientific papers
Kras-G12C inhibitor heterocyclic compounds
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Paragraph 0217; 0220-0223, (2021/06/23)
The invention relates to Kras-G12C inhibitor heterocyclic compounds represented by formula I, a preparation method thereof, and application of the Kras-G12C inhibitor heterocyclic compounds in prevention and treatment of tumor diseases such as lung cancer, colorectal cancer and pancreatic cancer. In the preparation process, the compounds of the general formula I are obtained through a series of reactions such as SN2 reaction, protection, coupling reaction, deprotection, condensation reaction and the like.
Structure-activity relationships of trans-substituted-propenoic acid derivatives on the nicotinic acid receptor HCA2 (GPR109A)
Van Veldhoven,Blad,Artsen,Klopman,Wolfram,Abdelkadir,Lane,Brussee,Ijzerman
supporting information; experimental part, p. 2736 - 2739 (2011/06/20)
Nicotinic acid (niacin) has been used for decades as an antidyslipidemic drug in man. Its main target is the hydroxy-carboxylic acid receptor HCA2 (GPR109A), a G protein-coupled receptor. Other acids and esters such as methyl fumarate also interact with the receptor, which constituted the basis for the current study. We synthesized a novel series of substituted propenoic acids, such as fumaric acid esters, fumaric acid amides and cinnamic acid derivatives, and determined their affinities for the HCA2 receptor. We observed a rather restricted binding pocket on the receptor with trans-cinnamic acid being the largest planar ligand in our series with appreciable affinity for the receptor. Molecular modeling and analysis of the structure-activity relationships in the series suggest a planar trans-propenoic acid pharmacophore with a maximum length of 8 ? and out-of-plane orientation of the larger substituents.
Fumaric acid derivative and polymer therefrom
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, (2008/06/13)
A polymer obtained by polymerizing a fumaric acid derivative represented by the following general formula (1): STR1 in which R1 represents an alkyl group having 1-6 carbon atoms and A denotes a radical of STR2 in which R2 and R3 represent each an alkyl group having 1-4 carbon atoms and may be identical with or different from each other, R4 denotes an alkyl group having 1-6 carbon atoms or a benzyl group and m and n denote each an integer of 1-6.
Process for the preparation of fumaric acid monoesters
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, (2008/06/13)
Fumaric acid monoesters can be prepared by introducing a hydroxyl compound at a rate corresponding to the progress of the reaction into a solution or a melt of maleic anhydride, which may optionally be substituted, if appropriate in the presence of a cis-trans catalyst. New fumaric acid monoesters can be formed by the process.
