cas 19473-96-2, 1-methyl 4-(2-carboxyvinyl)benzoate

Articles about 19473-96-2Total 10 be found

Histone deacetylase inhibitor as well as preparation and application thereof
The invention relates to a histone deacetylase inhibitor and preparation and an application thereof, in particular to a novel histone deacetylase inhibitor based on a beta-elemene structure and a preparation method thereof, and further relates to an intermediate for synthesizing the histone deacetylase inhibitor and a preparation method thereof. The invention also relates to an application of the histone deacetylase inhibitor in preparation of antitumor drugs, and belongs to the technical field of chemical synthesis of drugs. The zinc ion combined compound and the salt or solvate thereof are shown as a general formula (I) or (II), wherein R, X, n and i are described in the claims and the specification.
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Paragraph 0044-0045

(2021/04/28)

Discovery of Novel Benzothiazepinones as Irreversible Covalent Glycogen Synthase Kinase 3β Inhibitors for the Treatment of Acute Promyelocytic Leukemia
Recently, irreversible inhibitors have attracted great interest in antitumors due to their advantages of forming covalent bonds to target proteins. Herein, some benzothiazepinone compounds (BTZs) have been designed and synthesized as novel covalent GSK-3β inhibitors with high selectivity for the kinase panel. The irreversible covalent binding mode was identified by kinetics and mass spectrometry, and the main labeled residue was confirmed to be the unique Cys14 that exists only in GSK-3β. The candidate 4-3 (IC50 = 6.6 μM) showed good proliferation inhibition and apoptosis-inducing ability to leukemia cell lines, low cytotoxicity on normal cell lines, and no hERG inhibition, which hinted the potential efficacy and safety. Furthermore, 4-3 exhibited decent pharmacokinetic properties in vivo and remarkably inhibited tumor growth in the acute promyelocytic leukemia (APL) mouse model. All the results suggest that these newly irreversible BTZ compounds might be useful in the treatment of cancer such as APL.
Zhang, Peng,Min, Zhihui,Gao, Yang,Bian, Jiang,Lin, Xin,He, Jie,Ye, Deyong,Li, Yilin,Peng, Chao,Cheng, Yunfeng,Chu, Yong
p. 7341 - 7358
(2021/06/28)

Acrylamide benzoazepine derivatives as GSK-3beta inhibitors and applications thereof
The invention belongs to the technical field of medicinal chemistry, and discloses acrylamide benzoazepine derivatives serving as glycogen synthase kinase-3beta (GSK-3beta) inhibitors and applicationsof the acrylamide benzoaza derivatives. The derivatives are compounds shown as a formula (I) or pharmaceutically acceptable salts thereof. The compounds have good inhibitory activity on GSK-3beta andcan be used as selective inhibitors for preventing and treating GSK-3beta-related diseases, and the GSK-3beta-related diseases include cancer, neurodegenerative diseases and diabetes.
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Paragraph 0051-0054

(2020/11/26)

Five-membered azole-containing heterocyclic chalcone derivative, and preparation method and medical use thereof
The invention discloses a five-membered azole-containing heterocyclic chalcone derivative, and a preparation method and a medical use thereof. The five-membered azole-containing heterocyclic chalconederivative is represented by general formula (I) shown in the description, and R1 in the is formula (I) is any one of formulas also shown in the description. A result of antitumor cell proliferation activity detection shows that the above compound has a certain inhibitory effect on the proliferation of lung cancer A549 and breast cancer MCF-7 cells, and can be used as an antitumor drug.
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(2019/06/30)

Preparation method of pemetrexed acid
Belonging to the technical field of organic compound synthesis, the invention in particular relates to a preparation method of pemetrexed acid. The method is characterized by utilizing methyl p-formylbenzoate and malonic acid as the starting materials to synthesize the target product. Compared with the methods for synthesis of the compound reported in previous literatures, the method provided by the invention has the advantages of easily available raw materials, low price and no pollution, greatly reduces the production cost, and is suitable for large-scale industrial production. The method isa brand new synthetic route for the compound.
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Paragraph 0043; 0044

(2019/05/16)

Unexpected CO2 splitting reactions to form CO with N-heterocyclic carbenes as organocatalysts and aromatic aldehydes as oxygen acceptors
(Chemical Equation Presented) The catalytic reduction of carbon dioxide to carbon monoxide under mild conditions using aromatic aldehydes as reductants and NHCs as organocatalysts was developed. This carbon dioxide splitting reaction provides a new method for metal-free carbon dioxide reduction and steps forward in utilizing carbon dioxide as a renewable "green" source under mild conditions. On the other hand, this reaction also shows a new economical way to oxidize aromatic aldehydes under mild conditions with carbon dioxide and could be applied in pharmaceutical synthesis.
Gu, Liuqun,Zhang, Yugen
supporting information; experimental part
p. 914 - 915
(2010/04/01)

INHIBITORS OF HISTONE DEACETYLASE
The invention provides compoods and methods for treating cell proliferative- diseases. The invention provides new inhibitors of histone deacetylase enzymatic activity, compositions of the compounds comprising the inhibitors and a pharmaceutically acceptable carrier, excipient, or diluent, and methods of using the compounds to inhibit cellular proliferation in vitro and therapeutically.
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Page 33

(2008/06/13)

Thiazole derivative
A thiazole compound of the formula: STR1 wherein T is lower alkylene; u is 0 or 1; R1 and R2 are the same or different and are each H, or lower alkyl, etc.; R3 is STR2 R4 is H or lower alkanoyloxy-lower alkyl, which shows inhibitory activity on protein kinase C (PKC, Ca2+ /phospholipid-depending serine/threonine protein phosphatase), and are useful as a protein kinase C inhibitor.
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(2008/06/13)

PHOTOSYNTHESIS OF HETEROPOLYCYCLIC QUINOLONES
Four new anilidoquinolones; 9-anilidobenzothienoquinolin-6(5H)-one (6), 9-N'-methylanilidobenzothieno-5-N-methylquinolin-6-one (7), 9-anilidothienothienylquinolin-6(5H)-one (16), and 9-N'-methylanilidothienothienyl-5-N-methylquinolin-6-one (17) were prepared by photochemical dehydrohalogenation from the dianilides (4,5,14 and 15).Photochemical dehydrogenation of the anilides to produce multicondensed diquinolones did not occur.
Dogan, Jasna,Karminski-Zamola, Grace M.,Boykin, David W.
p. 1659 - 1666
(2007/10/03)