15 research outputs found
Effects of implant length and 3D bone-to-implant contact on initial stabilities of dental implant: a microcomputed tomography study
Numerical assessment of bone remodeling around conventionally and early loaded titanium and titanium–zirconium alloy dental implants
Anti-tumor effects of a novel retinoic acid metabolism blocking agent VN/14-1 in the N-methyl-N-nitrosourea-induced rat mammary carcinoma model and its effects on the uterus
Chemical activation of RARβ induces post-embryonically bilateral limb duplication during Xenopus limb regeneration
Novel Tetralone-Derived Retinoic Acid Metabolism Blocking Agents: Synthesis and in Vitro Evaluation with Liver Microsomal and MCF-7 CYP26A1 Cell Assays
Small MolecuImidazole Methyl 3-(4-(aryl-2-ylamino)phenyl)propanoates
The synthesis and potent inhibitory activity of novel imidazole methyl 3-(4-(aryl-2-ylamino)phenyl)propanoates in a MCF-7 CYP26A1 microsomal assay is described. The induction of CYP26A1 mRNA was used to evaluate the ability of the compounds to enhance the biological effects of all-trans retinoic acid (ATRA) in a retinoid-responsive neuroblastoma cell line. The most promising inhibitor, 3-imidazol-1-yl-2-methyl-3-[4-(naphthalen-2-ylamino)-phenyl]-propionic acid methyl ester (20), with an IC50 of 3 nM (compared with liarozole IC50 of 540 nM and R116010 IC50 of 10 nM) was further evaluated for CYP selectivity using a panel of CYP enzymes, mutagenicity (Ames screen), and hepatic stability