29096-64-8Relevant academic research and scientific papers
DERIVATIVES OF 4-(IMIDAZO[L,2-A]PYRIDIN-3-YL)-N-(PYRIDINYL)PYRIMIDIN- 2-AMINE AS THERAPEUTIC AGENTS
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Paragraph 0083-0084; 0096, (2021/01/29)
A novel class of heteroaryl compounds for use in the prevention and/or treatment of proliferative diseases and conditions including cancers. The compounds are considered to be capable of inhibiting cell proliferation by inhibiting the activity of FLT3 and its mutant forms and/or other protein kinases such as CDKs. The compounds have the general structure I:
Discovery and Characterization of Selective and Ligand-Efficient DYRK Inhibitors
Ashall-Kelly, Alexander,Bennett, James,Elkins, Jonathan M.,Fedorov, Oleg,Godoi, Paulo H.,Hanley, Marcus T.,Henderson, Scott H.,Hopkins Navratilova, Iva,Robinson, Sean,Ruela De Sousa, Roberta,Sorrell, Fiona,Walter, Daryl S.,Ward, Simon E.
supporting information, p. 11709 - 11728 (2021/08/24)
Dual-specificity tyrosine-regulated kinase 1A (DYRK1A) regulates the proliferation and differentiation of neuronal progenitor cells during brain development. Consequently, DYRK1A has attracted interest as a target for the treatment of neurodegenerative diseases, including Alzheimer's disease (AD) and Down's syndrome. Recently, the inhibition of DYRK1A has been investigated as a potential treatment for diabetes, while DYRK1A's role as a mediator in the cell cycle has garnered interest in oncologic indications. Structure-activity relationship (SAR) analysis in combination with high-resolution X-ray crystallography leads to a series of pyrazolo[1,5-b]pyridazine inhibitors with excellent ligand efficiencies, good physicochemical properties, and a high degree of selectivity over the kinome. Compound 11 exhibited good permeability and cellular activity without P-glycoprotein liability, extending the utility of 11 in an in vivo setting. These pyrazolo[1,5-b]pyridazines are a viable lead series in the discovery of new therapies for the treatment of diseases linked to DYRK1A function.
1,5-DIHYDRO-2H-PYRROL-2-ONE COMPOUNDS AND METHODS OF USING SAME
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Paragraph 0382-0395, (2018/08/20)
The present invention relates to 1,5-dihydro-2H-pyrrol-2-one compounds and methods of using them to induce self-renewal of stem/progenitor supporting cells, including inducing the stem/progenitor cells to proliferate while maintaining, in the daughter cells, the capacity to differentiate into tissue cells.
Double (amino-sulfur generation of formic acid ) - 1,3-propane diester compound and its synthetic method, pharmaceutical composition and use thereof
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Paragraph 0310-0313, (2016/10/08)
The invention relates to a bis(aminodithioformate)-1,3-propane diester compound, and synthesis method thereof, a pharmaceutical composition containing the compound and a use, and especially relates to the use in preparing drugs for treating or preventing cancers. The compound is represented as the formula (I), wherein A is selected from substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heterocyclic group, R1 and R2 are the same or different and are independently selected from hydrogen, alkyl, aryl alkyl or heteroaryl alkyl, or a substituted or unsubstituted heterocyclic ring formed together by the R1, the R2 and an N atom connected with the R1 and the R2.
A 2-amino-thiazole compounds (by machine translation)
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Paragraph 0223-0225, (2016/10/08)
The present invention relates to the technical field of pharmaceutical chemistry, particularly relates to a 2-amino thiazole compound or its pharmaceutically acceptable salts, its preparation method, and pharmaceutical compositions containing such compounds and its application in the preparation of antineoplastic. (by machine translation)
Discovery and optimization of novel dual dithiocarbamates as potent anticancer agents
Li, Ri-Dong,Wang, Hui-Ling,Li, Ying-Bo,Wang, Zhong-Qing,Wang, Xin,Wang, Yi-Tao,Ge, Ze-Mei,Li, Run-Tao
, p. 381 - 391 (2015/03/04)
A series of dual dithiocarbamates were synthesized and evaluated for their in-vitro anticancer activities on human non-small cell lung cancer cell line H460. Nine compounds exhibited significant antiproliferative activities with IC50 less than 1 μM. Among them, compound 14m showed the highest inhibitory activity against H460 cell and inhibited the growth of nine types of tumor cells with IC50 values less than 1 μM. It also achieved IC50 of 54 nM and 23 nM against HepG2 and MCF-7 cell lines, respectively. Preliminary structure-activity relationship study indicated that: a) when the methyl group (region A) is substituted with benzene rings, ortho substitution on the benzene ring is favored for activity; b) substitution with heterocyclic structures at region A exhibited greater impact on the anti-tumor activity of compounds, in which pyridine ring, thiazole ring, coumarin and benzo[b]thiophene are favored and quinoline ring is the most favored; c) substitution with different amines (region B) also showed marked effect on the activity of compounds and dimethylamine and morpholine are preferred to other tested amines.
Arylpiperazines as fatty acid transport protein 1 (FATP1) inhibitors with improved potency and pharmacokinetic properties
Matsufuji, Tetsuyoshi,Ikeda, Mika,Naito, Asuka,Hirouchi, Masakazu,Kanda, Shoichi,Izumi, Masanori,Harada, Jun,Shinozuka, Tsuyoshi
, p. 2560 - 2565 (2013/07/04)
The discovery and optimization of a novel series of FATP1 inhibitors are described. Through the derivatization process, arylpiperazine derivatives 5k and 12a were identified as possessing potent in vitro activity against human and mouse FATP1s as well as
FUSED HETEROCYCLYC INHIBITOR COMPOUNDS
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Page/Page column 65, (2010/03/02)
The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) and/or Cyclin-dependent kinase (CDK) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound
NOVEL SUBSTITUTED IMIDAZOLE DERIVATIVES
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Page/Page column 44, (2010/11/27)
The present invention relates to a compound represented by Formula [I] or a pharmaceutically acceptable salt or ester thereof: wherein: X1, X2, X3, and X4, which may be identical or different, are each C or N, provided that none to two of X1, X2, X3, and X4 is/are N; Y is CH or N; R1, R1', R2, R2', R3, R3', R4, and R4', which may be identical or different, are each a hydrogen atom, a lower alkyl group, or the like; R5 is a hydrogen atom or a methyl group; R6 and R7, which may be identical or different, are each a hydrogen atom, a lower alkyl group, or the like; R8 and R8', which may be identical or different, are each a hydrogen atom, a lower alkyl group, or the like; R9 is an aryl group or a heteroaryl group which may be substituted; and n is an integer from 1 to 3, and a PLK1 inhibitor or an anticancer agent containing the same.
Imidazo[1,2-a]pyridines. Part 2: SAR and optimisation of a potent and selective class of cyclin-dependent kinase inhibitors
Byth, Kate F.,Culshaw, Janet D.,Green, Stephen,Oakes, Sandra E.,Thomas, Andrew P.
, p. 2245 - 2248 (2007/10/03)
Exploration of SAR and optimisation of the imidazo[1,2-a]pyridine CDK inhibitors has lead to the discovery of novel, potent and selective inhibitors of the cyclin-dependent kinase CDK2. Understanding of SAR has identified positions of substitution, which allow modification of physical properties and offer the potential for in vivo optimisation.
