Book excerpt: pH Interfering Agents as Chemosensitizers In Cancer Therapy, Volume Thirteen, provides a detailed overview of the chemosensitizers for the treatment of cancer spanning from biochemical and structural features to pharmacology and drug-design, including technological applications. The book is structured with innovative outlines and a distinction between experimental and clinical results. The continuous discovery and assessment of the role played by old/new synthetic drugs, natural compounds and technological applications has led to the urgent need of classification in terms of biological activity, mechanism of action, clinical outcomes, cancer cell lines sensible to the treatment, and potentialities to better orient research in this field. Moreover, all the aspects relevant for medicinal chemistry (drug design, structure-activity relationships, permeability data, cytotoxicity, appropriate statistical procedures, and molecular modeling studies) are strictly considered. - Presents a broad view of the topic according to a medicinal chemistry-based approach beyond syntheses and biological assays, focusing on SAR studies, chemoinformatic, drug targeting and molecular modeling - Explains the mechanism of action of the chemosensitizers by means of schemes and figures to facilitate comprehension - Discusses novel targets to explore new possibilities that enhance research in the field