Recent Advances in chemistry and pharmacology of 2-methoxyestradiol: An anticancer investigational drug

•Chemistry, Biochemistry and pharmacological profile of 2-methoxyestradiol.•Chemistry-total syntheses, derivatives and analytical techniques for quantification.•Pharmacology-anticancer, SAR, mechanism of action, toxicity, pharmacokinetics.

2-Methoxyestradiol (2ME2), an estrogen hormone metabolite is a potential cancer chemotherapeutic agent. Presently, it is an investigational drug under various phases of clinical trials alone or in combination therapy. Its anticancer activity has been attributed to its antitubulin, antiangiogenic, pro-apoptotic and ROS induction properties. This anticancer drug candidate has been explored extensively in last twenty years for its detailed chemistry and pharmacology. Present review is an update of its chemistry and biological activity. It also extends an assessment of potential of 2ME2 and its analogues as possible anticancer drug in future.

Graphical abstractAn update of chemistry and pharmacology of 2-methoxyestradiol.Figure optionsDownload full-size imageDownload as PowerPoint slide