Tubulin inhibitors: a patent review

Abstract

Introduction: Microtubules play an important role in several cellular processes, particularly in the formation of the mitotic spindle during the process of mitosis. These highly dynamic mitotic-spindle microtubules have become a successful target of cancer therapy. Microtubule-targeting agents, such as vinca alkaloids and taxanes, were used in clinic over 50 years. In past decades, development of new antimicrotubule agents that possess different structure and binding sites of tubulin has shown potent activity against the proliferation of various cancer cells, as well as in multidrug-resistant cancers. Interestingly, many of these agents represent an attractive ability that targeting the tumor blood vessels results in tumor vascular disruption. Therefore, exploring new agents and strategies may provide more effective therapeutic options in the related treatment of cancer.

Areas covered: In past few years, there are many chemical compounds that successfully interferes the microtubules and display antitumor effect. In these, published compounds supply the fresh minds in modification of present drugs and new insights into the development of tubulin inhibitors.

Expert opinion: This article arranges the microtubule-targeting agents that have published in patent in recent years. It may help in the investigation of new tubulin binding site and development of novel drug candidate in the future.