Anticancer Drugs

Steroidal aromatase inhibitors type I inhibitors

Aromatase inhibitors are normally classified as steroidal (type I) or nonsteroidal (type II). Numerous steroidal agents have been developed that exhibit either competitive inhibition, irreversible inhibition, or mechanism-based inhibition of aromatase.24 Mechanism-based inhibitors are bound to the catalytic site of the enzyme, which transforms them into electrophilic intermediates that become irreversibly attached to the enzyme, blocking its activity, and they are known as ''aromatase...

Anticancer Drugs Targeting Tubulin and Microtubules

Drugs That Inhibit Microtubule Polymerization at High Concentrations 231 2.1. Compounds binding at the Vinca site 231 2.2. Compounds binding at the colchicine site 236 3. Microtubule-Stabilizing Agents Compounds Binding at the 3.3. Miscellaneous marine compounds that bind to 4. Miscellaneous Anticancer Drugs Acting 5. Antivascular Effects of Microtubule-Targeted Agents 245 6. Mitotic Kinesin Inhibitors 246 References 247 Microtubules are filamentous intracellular structures that are responsible...

Anthracyclines And Their Analogs

Anthracyclines are a group of antibiotics characterized by the presence of a planar chromophore containing an anthraquinone fragment, attached to an amino sugar. Daunomycin or daunorubicin (DNR) and doxorubicin (DOX), previously called adriamycin, were isolated from a Streptomyces species and were the first anthracycline antibiotics introduced in the clinic for cancer treatment. They are widely used for the treatment of human cancers, and, despite its very similar structure, their antitumor...

Epigenetic Therapy Of Cancer

The initiation and progression of cancer is controlled by both genetic and epige-netic events. The term ''epigenetic'' refers to alterations in gene expression that are not associated with changes in DNA sequence. Unlike genetic alterations, epigenetic aberrations are potentially reversible. The best studied epigenetic alterations are DNA methylation and histone tail modifications, and epigenetic gene silencing by these mechanisms has become an attractive anticancer target.51 The main enzymes...