Marine Derived Anticancer Drugs Targeting Microtubule.

BACKGROUND: Microtubule dynamics plays a vital role in regulating crucial cellular functions and is one of the most attractive anticancer drug targets. Microtubule targeting agents (MTAs) such as the vinca alkaloids or taxanes, although are effective for cancer therapy, have adverse side effects. Another hindrance in their development is multiple drug resistance in tumor cells. These drawbacks have urged the need to develop novel MTAs from alternative sources, with better therapeutic efficacy. Recently, MTAs from marine sources have grabbed much attention due to unique tubulin binding features and remarkable ability to reduce tumor progression.

OBJECTIVE: The emphasis of the article is to provide an overview of some of the most promising marine derived MTAs and highlight their major characteristics in brief.

METHOD: Patent databases such as USPTO, Espacenet and WIPO were searched systematically for recent patents published from 2006 up to 2016. Numerous data retrieved was analyzed critically, and only those patents focusing on the chemical synthesis and/or modifications of marine derived MTAs along with a significant demonstration of their in vitro and/or in vivo activity are summarized here.

RESULTS: Some of the marine derived MTAs have significant antiproliferative potency against a wide array of cancers and are also able to overcome multidrug resistance.

CONCLUSION: The marine derived MTAs hold great potential in the field of cancer therapeutics and are gradually advancing in the clinical set up. A deeper understanding of the molecular mechanisms combined with innovative therapeutic regimen would lead to major advances in the field.