Tubulin and Microtubules as Drug Targets for Potential Cancer Chemotherapy and CNS-Directed TherapiesMicrotubules are essential cellular constituents of eukaryotes formed by tubulin subunits. This book is a collection of medicinal chemistry research projects that utilizes microtubules as drug targets for human diseases of global health impact. The main chapters (2 – 4) include an in-depth description of different synthetic and biological approaches to characterize the therapeutic potential of novel synthetic molecules for cancer, Alzheimer’s disease, and neglected tropical diseases. This book also includes three short chapters (5 – 7) of additional collaborative projects focused on varied drug discovery topics, including SAR studies of new lead compounds targeting carbonic anhydrase enzymes, FAAH and TRPV1, and novel bioisosteres of the carboxylic acid functional group. |
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13C NMR ¹H NMR acid activity added afforded the title agents Alzheimer’s disease Anal analysis assay ATIs binding Biol brain calculated cancer CDCl3 changes Chem cm-¹ colchicine column chromatography hexanes/EtOAc concentrations crystallization derivatives determined disappeared on treatment DMSO-d6 drug dynamics effect equiv EtOH evaluated expression Figure Following synthetic procedure function gel column chromatography growth HRMS ES+ human ibuprofen increased inhibition inhibitors interactions layer levels mechanism microtubule mitotic mixture mmol MT-stabilizing NMR 400 MHz obtained organic paclitaxel polymerization potential protein purification by silica reaction represent ring showed silica gel column solution stability stirred structure studies Synthesis Table temperature test compounds tion title compound treat treatment with D2O TRPV1 tubulin values white solid yellow solid yield