80407-64-3Relevant articles and documents
The influence of polyether substituents on biological activity of curcumin derivatives
Deptula, Tomasz,Krwczyski, Adam,Bubko, Irena,Gruber-Bzura, Beata Maria
, p. 99 - 111 (2020/04/10)
Curcumin is reported as an anti-proliferative and chemopreventive compound. However, it shows poor water solubility, low bioavailability, and rapid metabolism. To address these problems, curcumin derivatives substituted with polyether chain were synthesiz
Styryl xanthine derivatives and uses thereof (by machine translation)
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Paragraph 0174; 0180; 0181; 0182; 0218; 0219; 0220, (2019/08/02)
The invention discloses styryl xanthine derivatives and application, and particularly, relates to a novel styryl xanthine derivative and a pharmaceutical composition containing the same, and can be used as selective adenosine A. 2A Are antagoni
Preparation method of erlotinib hydrochloride intermediate
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, (2019/05/08)
The invention provides a preparation method of an erlotinib hydrochloride intermediate. The preparation method comprises following steps: removing the methyl of vanillin, performing esterification, converting an aldehyde group into a nitrile group, and carrying out nitration, reduction, hydrolysis, and ring forming reactions. The reaction route is represented in the description. The technology isreasonable, the operation is simple, the cost is low, and the reaction yield is high.
Preparation method of erlotinib intermediate
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, (2016/10/10)
The invention relates to a preparation method of an erlotinib intermediate. The method concretely comprises the following steps: 1, dissolving vanillin in an organic solvent I, adding aluminum trichloride, adding pyridine in a dropwise manner, and reacting to obtain ELTA; 2, dissolving the ELTA in an organic solvent II, adding 2-chloroethylmethyl ether, potassium carbonate and a phase transfer catalyst, and reacting to obtain ELTB; 3, adding the ELTB to water, adding an alkali and potassium permanganate, and reacting to obtain ELTC; 4, adding concentrated sulfuric acid to methanol in a dropwise manner, adding the ELTC to the above reaction system, and reacting to obtain ELTD; 5, adding concentrated sulfuric acid to concentrated nitric acid in a dropwise manner, dissolving the ELTD in an organic solvent IV, adding a prepared mixed acid to the reaction system, and reacting to obtain ELTE; 6, adding the ELTE, iron powder and ammonium chloride to an organic solvent V, adding concentrated hydrochloric acid in a dropwise manner, and reacting to obtain ELTF; and 7, adding the ELTF, trimethyl orthoformate and ammonium acetate to an organic solvent VI, and reacting to obtain the erlotinib intermediate.
CARBOXYLIC ACID ARYL AMIDES
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Page/Page column 23; 24, (2012/07/28)
Compounds of formula and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of proliferative diseases, including cancer.
NOVEL PYRAZOLO [3, 4 -D] PYRIMIDINE DERIVATIVES AS ANTI-CANCER AGENTS
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Page/Page column 35, (2010/12/29)
The invention relates to substituted pyrazolo[3,4-d]pyrimidine derivatives of the Formula-(I), or pharmaceutically acceptable salts thereof, which possess anti-proliferative activity such as anti-cancer activity and are accordingly useful in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of substituted pyrazolo[3,4-d]pyrimidine derivatives, to pharmaceutical compositions containing the compound and to its use in the manufacture of medicaments for the production of an anti-proliferative effect in a warm-blooded animal such as man
ISOQUINOLINE AMINOPYRAZOLE DERIVATIVES, THEIR MANUFACTURE AND USE AS PHARMACEUTICAL AGENTS FOR THE TREATMENT OF CANCER
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Page/Page column 83-84, (2008/06/13)
Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
A Comparison of the Inhibitory Action of 5-(Substituted-benzyl)-2,4-diaminopyrimidines on Dihydrofolate Reductase from Chicken Liver with That from Bovine Liver
Li, Ren-li,Hansch, Corwin,Kaufman, Bernard T.
, p. 435 - 440 (2007/10/02)
Forty-four 5-(substituted-benzyl)-2,4-diaminopyrimidines have been tested as inhibitors of chicken and bovine liver dihydrofolate reductase.The chicken enzyme is, on the average, about 10 times less easily inhibited than bovine enzyme.Substituents which show the greatest selectivity are 4-NHCOCH3, 3-OC4H9, 3-I, 3-CF3-4-OCH3, and 3,4,5-(OCH3)3.The inhibition constants have been used to formulate quantitative structure-activity relationships for comparative purposes.