331845-86-4Relevant academic research and scientific papers
Aniline pyrimidines, its preparation method and medical use (by machine translation)
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Paragraph 0323; 0324; 0325, (2018/03/01)
The invention relates to: an aniline pyrimidine compound represented as the formula (I), a medicinal salt thereof, a prodrug thereof, and a hydrate or solvate thereof and also relates to: the preparation method of the compound, a medicine composition comp
Synthesis and structure-activity relationship of (E)-phenoxyacrylic amide derivatives as Hypoxia-Inducible Factor (HIF) 1α inhibitors
Naik, Ravi,Won, Misun,Kim, Bo-Kyung,Xia, Yan,Choi, Hyun Kyung,Jin, Guanghai,Jung, Youngjin,Kim, Hwan Mook,Lee, Kyeong
supporting information, p. 10564 - 10571 (2013/02/22)
A series of (E)-phenoxyacrylic amide derivatives were synthesized and evaluated as hypoxia inducible factor (HIF) 1α inhibitors. The present structure-activity relationship study on this series identified the morpholinoethyl containing ester 4p as a potent inhibitor of HIF-1α under hypoxic conditions (IC50 = 0.12 μM in a cell-based HRE reporter assay) in HCT116 cells. The representative compound 4p suppressed hypoxia-induced HIF-1α accumulation and targeted gene expression in a dose-dependent manner. The effect of HIF-1α inhibition by 4p was further demonstrated by its inhibitory activity on in vitro tube formation and migration of cells, which may be valuable for development of novel therapeutics for cancer and tumor angiogenesis.
Exploration of secondary and tertiary pharmacophores in unsymmetrical N,N′-diaryl urea inhibitors of soluble epoxide hydrolase
Anandan, Sampath-Kumar,Gless, Richard D.
scheme or table, p. 2740 - 2744 (2010/07/15)
The impact of various secondary and tertiary pharmacophores on in vitro potency of soluble epoxide hydrolase (sEH) inhibitors based on the unsymmetrical urea scaffold 1 is discussed. N,N′-Diaryl urea inhibitors of soluble epoxide hydrolase exhibit subtle variations in inhibitory potency depending on the secondary pharmacophore but tolerate considerable structural variation in the second linker/tertiary pharmacophore fragment.
5-OXO-5,8-DIHYDRO-PYRIDO-PYRIMIDINES AS INHIBITORS OF C-FMS KINASE
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Page/Page column 127, (2008/12/05)
The invention addresses the current need for selective and potent protein tyrosine kinase inhibitors by providing potent inhibitors of c-fms kinase. The invention is directed to the novel compounds of Formula I: or a salt, stereoisomer, tautomer, crystalline, polymorph, amorphous, solvate, hydrate, ester, prodrug or metabolite form thereof, wherein A, Y, Z, R101 and R200 are described in the specification.
A novel approach for the synthesis of aryl amides
Shaabani, Ahmad,Soleimani, Ebrahim,Rezayan, Ali Hossein
, p. 6137 - 6141 (2008/03/12)
A novel and highly efficient approach for the synthesis of aryl amides in high yields by the reaction of carboxylic acids and isocyanides in methanol at ambient temperature is reported.
