56966-63-3Relevant articles and documents
N2,N4-BIS(4-(PIPERAZINE-1-YL)PHENYL)PIRIMIDINE-2,4-DIAMINE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, AND COMPOSITION CONTAINING SAME AS ACTIVE INGREDIENT FOR PREVENTING OR TREATING CANCER
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Paragraph 0087, (2015/07/02)
The present invention relates to a N2,N4-bis(4-(piperazine-1-yl)phenyl)pirimidine-2,4-diamine derivative or a pharmaceutically acceptable salt thereof, and to a composition containing same as an active ingredient for preventing or treating cancer. Since the compound according to the present invention has good effects in inhibiting the activities of anaplastic lymphoma kinase (ALK) and activated Cdc42-associated kinase (ACK1), the compound can have improved therapeutic effects against cancer cells having ALK fusion proteins such as EML4-ALK and NPM-ALK and is expected to be effective in preventing the recurrence of cancer. Therefore, the compound can be effectively used as a composition for preventing or treating cancer.
Ortho-selectivity in SNAr substitutions of 2,4-dihaloaromatic compounds. Reactions with anionic nucleophiles
Wendt, Michael D.,Kunzer, Aaron R.
scheme or table, p. 3041 - 3044 (2010/07/18)
The nucleophilic addition of organic anions to aromatic compounds with halogens positioned both ortho and para to activating groups was studied in a variety of solvents. Substrates showed strong preferences for ortho substitution in most cases. Evidence is presented for activating group-dependent coordination, which contributes to very high ortho-selectivity in nonpolar solvents. This also drives the overall reaction rate in these solvents, and is of close to the same magnitude of rate increase derived from polar solvents. para-Products are maximized by using crown ethers in protic solvents. Solvent effects overall are very different from corresponding reactions with amine nucleophiles due primarily to the different charges present in the transition states, and to solvation of the nucleophile.
Design, synthesis and structure-affinity relationships of aryloxyanilide derivatives as novel peripheral benzodiazepine receptor ligands
Okubo, Taketoshi,Yoshikawa, Ryoko,Chaki, Shigeyuki,Okuyama, Shigeru,Nakazato, Atsuro
, p. 423 - 438 (2007/10/03)
Since the peripheral benzodiazepine receptor (PBR) has been primarily found as a high-affinity binding site for diazepam in rat kidney, numerous studies of it have been performed. However, the physiological role and functions of PBR have not been fully elucidated. Currently, we presented the pharmacological profile of two high and selective PBR ligands, N-(2,5-dimethoxybenzyl)-N-(4-fluoro-2-phenoxyphenyl)acetamide (7-096, DAA1106) (PBR: IC50=0.28 nM) and N-(4-chloro-2-phenoxyphenyl)-N-(2- isopropoxybenzyl)acetamide (7-099, DAA1097) (PBR: IC50=0.92 nM). The compounds are aryloxyanilide derivatives, and identified with known PBR ligands such as benzodiazepine (1, Ro5-4864), isoquinoline (2, PK11195), imidazopyridine (3, Alpidem), and indole (5, FGIN-1-27) derivatives. The aryloxyanilide derivatives, which have been derived by opening the diazepine ring of 1, are a novel class as PBR ligands and have exhibited high and selective affinity for peripheral benzodiazepine receptors (PBRs). These novel derivatives would be useful for exploring the functions of PBR. In this paper, the design, synthesis and structure-affinity relationships of aryloxyanilide derivatives are described.
