Publications (109) View all
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Article: Small-animal PET evaluation of [<sup>11</sup>C]MC113 as a PET tracer for P-glycoprotein
BMC Pharmacology. 01/2010; -
Article: A benzopyrane derivative as a P-glycoprotein stimulator: a potential agent to decrease β-amyloid accumulation in Alzheimer's disease.
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ABSTRACT: A simulating interaction: The P-glycoprotein (P-gp) ligand 13 displays high P-gp interacting activity (EC(50) =2.90 μM) and selectivity in tumor cell lines. Here, this promising compound was further evaluated ex vivo in an everted gut sac assay and found to behave as a P-gp stimulator, making this agent a potential lead for the development of new therapeutics to treat Alzheimer's disease.ChemMedChem 12/2011; 7(3):391-5. · 3.15 Impact Factor -
Article: Synthesis and toxicopharmacological evaluation of m-hydroxymexiletine, the first metabolite of mexiletine more potent than the parent compound on voltage-gated sodium channels.
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ABSTRACT: The first synthesis of m-hydroxymexiletine (MHM) has been accomplished. MHM displayed hNav1.5 sodium channel blocking activity, and tests indicate it to be ∼2-fold more potent than the parent mexiletine and to have more favorable toxicological properties than mexiletine. Thus, MHM and possible related prodrugs might be studied as agents for the treatment of arrhythmias, neuropathic pain, and myotonias in substitution of mexiletine (metabolite switch), which has turned out to be tainted with common toxicity.Journal of Medicinal Chemistry 12/2011; 55(3):1418-22. · 4.80 Impact Factor -
Article: Potent galloyl-based selective modulators targeting multidrug resistance associated protein 1 and P-glycoprotein.
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ABSTRACT: 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.Journal of Medicinal Chemistry 11/2011; 55(1):424-36. · 4.80 Impact Factor -
Article: Modulation, absorption and delivery of xenobiotics: the synergic role of CYP450 and P-gp activities.
Current Drug Metabolism 10/2011; 12(8):701. · 5.11 Impact Factor
