299950-93-9Relevant academic research and scientific papers
Design, synthesis, biological evaluation, NMR and DFT studies of structurally simplified trimethoxy benzamides as selective P-glycoprotein inhibitors: the role of molecular flatness
Stefanachi, Angela,Mangiatordi, Giuseppe Felice,Tardia, Piero,Alberga, Domenico,Leonetti, Francesco,Niso, Mauro,Colabufo, Nicola Antonio,Adamo, Carlo,Nicolotti, Orazio,Cellamare, Saverio
, p. 820 - 831 (2016)
In a recent investigation carried out on a panel of trimethoxybenzanilides, we showed that the formation of an intramolecular hydrogen bond is a key element for tuning P-gp inhibitory activity. In this study, we designed new structurally simplified trimet
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.
Solvent-dependent supramolecular assemblies of π-conjugated anion-responsive acyclic oligopyrroles
Maeda, Hiromitsu,Terashima, Yoshitaka
supporting information; experimental part, p. 7620 - 7622 (2011/09/15)
Amide-attached pyrrole-based π-conjugated anion receptors showed solvent-dependent assembled modes such as H-aggregates that were soluble in octane and highly organized structures that provided supramolecular gels in CH2Cl2 and 1,4-dioxane in the absence of π-π stacking.
