151029-72-0Relevant articles and documents
Design, synthesis, and evaluation of non-ATP-competitive small-molecule polo-like kinase 1 (Plk1) inhibitors
Chen, Dong-Xing,Huang, Jie,Liu, Meng,Xu, Yun-Gen,Jiang, Cheng
, p. 2 - 9 (2015)
A series of small-molecule Plk1 inhibitors targeting the substrate-binding pocket were designed through rational drug design for the first time. The designed compounds were synthesized and their activities were evaluated in vitro. Some of the targeted compounds showed potent Plk1 inhibitory activities and anti-proliferative characters. Particularly, 5i showed Plk1 inhibitory activity with an IC50 value of 0.68 μM. Compound 5i also showed cell growth inhibitory activity on HeLa cells with an IC50 value of 0.51 μM, which is about four times more potent compared to thymoquinone. The mechanism of action suggested that 5i was an ATP-independent and substrate-dependent Plk1 inhibitor. Compound 5i demonstrated excellent Plk1 inhibitory selectivity against Plk2, Plk3, and five serine/threonine and tyrosine kinases. Our discovery and structure-activity relationship study may provide useful lead compounds for further optimization of non-ATP-competitive Plk1 inhibitors.
BENZO FIVE-MEMBERED NITROGEN HETEROCYCLIC PIPERIDINE OR PIPERAZINE DERIVATIVES AND PREPARATION METHODS AND PHARMACEUTICAL COMPOSITIONS THEREOF
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Paragraph 0125, (2015/11/03)
This invention relates to a compound of formula (I) and its pharmaceutically acceptable salts: wherein R1, R2, X, Y, A, B are described in this patent specification. This invention also relates to the preparation methods of the compo
BENZISOXAZOLE PIPERIDINYL DERIVATIVES, PHARMACEUTICAL COMPOSITIONS COMPRISING THE DERIVATIVES AND THEIR USE
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Page/Page column 6; 10, (2012/01/03)
The invention relates to a benzisoxazolyl piperidine derivative having the following general formula, a salt or a hydrate thereof, wherein R, X, Y, R′ and T are defined as in the specification. Such compounds have serotonin system modulating effects such as antagonizing effect on 5-HT2A and inhibitory effect on 5-HT reuptake. The compounds have good analgesic and sedative activities with mild toxic and side effects. The invention also relates to a composition comprising said derivative and the use thereof.
Phenylpiperazine derivatives with a combination of partial dopamine-D2 receptor agonism and serotonin reuptake inhibition
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Page/Page column 21, (2010/11/08)
The invention relates to a group of novel phenylpiperazine derivatives with a dual mode of action: serotonin reuptake inhibition and partial agonism on dopamine-D2 receptors. The invention also relates to the use of a compound disclosed herein for the manufacture of a medicament giving a beneficial effect. The compounds have the general formula (1): wherein the symbols have the meanings given in the specification. and tautomers, stereoisomers and N-oxides thereof, as well as pharmacologically acceptable salts, hydrates and solvates of said compounds of formula (1) and its tautomers, stereoisomers and N-oxides.
Radical cyclisation onto imidazoles and benzimidazoles
Aldabbagh, Fawaz,Bowman, W. Russell
, p. 4109 - 4122 (2007/10/03)
New synthetic methodology has been developed for the synthesis of [1,2- a]fused imidazoles and benzimidazoles using intramolecular homolytic aromatic substitution. In the intramolecular substitution, N-(ω-alkyl) radicals are generated using Bu3SnH from N-(ω-phenylselanyl)alkyl side chains. Phenylselanyl groups are used as radical leaving groups to avoid problems in the N-alkylation of imidazoles and benzimidazoles. Arylsulfones for imidazoles, and phenylsulfides for benzimidazoles, are used at the leaving groups in the homolytic substitutions.
Agent for use as an anti-irritant
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, (2008/06/13)
The use of a compound having the formula STR1 or a cosmetically acceptable acid addition salt form thereof, for preventing or reducing irritation or itching of the skin of human beings; cosmetic compositions comprising said agents, processes for preparing
Hexitol derivatives having vasodilative activity
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, (2008/06/13)
Disclosed is a hexitol derivative represented by the formula (I): STR1 wherein Q represents a formula selected from the group consisting of STR2 wherein a represents NH, O or S; each of b, c and d independently represents CH or N; each of R1, R2, R3 and R4 independently represents hydrogen, lower alkyl, trifluoromethyl, aryl, lower alkanoyloxy, amino, lower alkylamino, lower alkanoylamino, lower alkanoyl, aroyl, halogen, nitro, (CH2)m OR 7, (CH2)m SR7, (CH2)m CO2 R7 where R7 represents hydrogen or lower alkyl and m represents an integer of 0 to 3; each of R5 and R6 independently represents hydrogen or lower alkyl; U represents >N-- or STR3 W represents a single bond, --O-- or --S--; X represents STR4 wherein each of Y1 and Y2 independently represents hydrogen, lower alkyl, hydroxyl, lower alkanoyloxy, nitrile or phenyl; or Y1 and Y2 are combined together to form oxygen; each of Y3 and Y4 independently represents hydrogen or lower alkyl; and l is an integer of 0 to 6, and where l is an integer of 2 to 6, each STR5 may be the same or different; Z represents hydrogen or nitro; and, n is 2 or 3 or a pharmaceutically acceptable salt thereof. The compounds show prominent coronary vasodilative activities, and are useful in treating angina pectoris and myocardial infarction.