405170-93-6Relevant articles and documents
Potent galloyl-based selective modulators targeting multidrug resistance associated protein 1 and P-glycoprotein
Pellicani, Raffaella Zoe,Stefanachi, Angela,Niso, Mauro,Carotti, Angelo,Leonetti, Francesco,Nicolotti, Orazio,Perrone, Roberto,Berardi, Francesco,Cellamare, Saverio,Colabufo, Nicola Antonio
supporting information; experimental part, p. 424 - 436 (2012/03/10)
The multifactorial nature of chemotherapy failure in controlling cancer is often associated with the occurrence of multidrug resistance (MDR), a phenomenon likely related to the increased expression of members of the ATP binding cassette (ABC) transporter superfamily. In this respect, the most extensively characterized MDR transporters include ABCB1 (also known as MDR1 or P-glycoprotein) and ABCC1 (also known as MRP1) whose inhibition remains a priority to circumvent drug resistance. Herein, we report how the simple galloyl benzamide scaffold can be easily and properly decorated for the preparation of either MRP1 or P-gp highly selective inhibitors. In particular, some gallamides and pyrogallol-1-monomethyl ethers showed remarkable affinity and selectivity toward MRP1. On the other hand, trimethyl ether galloyl anilides, with few exceptions, exhibited moderate to very high and selective P-gp inhibition.
INHIBITORS OF HISTONE DEACETYLASE
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Page/Page column 142, (2010/02/11)
The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
Inhibition of FGFR3 and treatment of multiple myeloma
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, (2008/06/13)
Methods of inhibiting fibroblast growth factor receptor 3 and treating various conditions mediated by fibroblast growth factor receptor 3 are provided that include administering to a subject a compound of Structure I, a pharmaceutically acceptable salt thereof, a tautomer thereof, or a pharmaceutically acceptable salt of the tautomer. Compounds having the Structure I have the following structure where and have the variables described herein. Such compounds may be used to prepare medicaments for use in inhibiting fibroblast growth factor receptor 3 and for use in treating conditions mediated by fibroblast growth factor receptor 3 such as multiple myeloma.