Book excerpt: Microtubules 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.