On September 25, 2014, Schwiebert, Erik; Streiff, John; Dixon, John; Gao, Hongwu; Ritchie, Joseph P.; Seales, Eric C.; Mai, Deborah published a patent.SDS of cas: 25813-24-5 The title of the patent was Preparation of coumarin thiazolyl derivatives and methods of use in treating hyperproliferative diseases. And the patent contained the following:
Coumarin thiazolyl derivatives I [R1 is H, halogen, OH, (un)substituted alkoxyl, (un)substituted amino, (un)substituted C1-6-alkyl, (un)substituted heterocycloalkyl; R2 is H, halogen, OH, NO2, CN, N3, thiocyanato, CF3, (un)substituted alkoxyl, (un)substituted amino, (un)substituted carbonyl, or (un)substituted C1-6-alkyl; R3 is H or substituted or unsubstituted C1-6-alkyl; R4 is (un)substituted C1-6-alkyl, (un)substituted aryl or (un)substituted heteroaryl; X is S or O; and, Y is O, NH or NMe] are provided. Thus, DBM-308 (II) was prepared from 3-chlorosalicylaldehyde via cyclocondensation with Et acetoacetate in EtOH containing piperidine to give 3-acetyl-8-chlorocoumarin (III); regioselective bromination with CuBr2 in CHCl3 to give 3-(bromoacetyl)-8-chlorocoumarin (IV); and cyclocondensation with 2-MeOC6H4NHC(:S)NH2 to give II. Methods for the treatment of hyperproliferative diseases, such as cancer, polycystic kidney disease, and fibrosis of different tissues (e.g., idiopathic pulmonary fibrosis), are provided. The antiproliferative activity of II was determined [GI50 = 166 nM; TGI = 247 nM; LC50 = >4,000 nM; IC50 = 0.69 μM vs. N828 cell line (hyperproliferative PKD cells); IC50 = 0.54 μM vs. 3-8C1 cell line (hyperproliferative PKD cells)]. The methods include administering to a subject a compound as described herein. Also provided are methods for inhibiting the interaction between two or more heat shock protein chaperones in a cell. The experimental process involved the reaction of 3,5-Dibromo-4-methoxypyridine(cas: 25813-24-5).SDS of cas: 25813-24-5
The Article related to coumarin thiazolyl derivative preparation treatment hyperproliferative disease, cancer treatment coumarin thiazolyl derivative, polycystic kidney disease treatment coumarin thiazolyl derivative, tissue fibrosis treatment coumarin thiazolyl derivative, idiopathic pulmonary fibrosis treatment coumarin thiazolyl derivative and other aspects.SDS of cas: 25813-24-5