112378-39-9Relevant articles and documents
Discovery of novel 4-aryl-thieno[1,4]diazepin-2-one derivatives targeting multiple protein kinases as anticancer agents
Lee, Junghun,Jung, Hoyong,Kim, Minjung,Lee, Eunkyu,Im, Daseul,Aman, Waqar,Hah, Jung-Mi
, p. 1628 - 1637 (2018)
A series of 4-aryl-thieno[1,4]diazepin-2-one were synthesized and evaluated for their antiproliferative activities against the A375P melanoma and U937 hematopoietic cell lines. Several compounds showed very potent antiproliferative activities toward both cell lines and the activities were better than that of sorafenib, the reference standard. Derivatives were made as amide (8a–8i, 9a–9m) and urea (10a–10d, 11a–11d) with diverse hydrophobic moieties. One of the most potent inhibitor 10d, 1-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-3-(4-(2-oxo-2,3-dihydro-1H-thieno [3,4-b][1,4]diazepin-4-yl)phenyl)urea was found to be very potent inhibitor of multi-protein kinases including FMS kinase (IC50 = 3.73 nM) and is a promising candidate for further development in therapeutics for cancer.
A 3-methyl-4-oxo-4 - (P-amino) phenyl-butyric acid
-
Paragraph 0053; 0054, (2016/12/07)
The invention discloses a preparation method of a levosimendan key intermediate 3-methyl-4-oxo-4-(p-amino)phenylbutyric acid, which comprises six reaction steps disclosed in the specification. The method has the advantages of novel technological design, accessible raw materials, environment-friendly reaction conditions, no need of virulent chemicals, high yield of each reaction step, high total yield and safe and simple operation, and is suitable for industrial production.
Microwave assisted rapid and efficient synthesis of aryl methyl ketones and β-keto esters using Meldrum's acid
More,Mahulikar
, p. 823 - 825 (2007/10/03)
Microwave mediated rapid and efficient synthesis of aryl methyl ketones and β-keto esters from acyl Meldrum's acid by hydrolysis and alcoholysis, respectively, has been reported.