Tubulin inhibitors as novel anticancer agents: an overview on patents (2013-2018)

Area of Science:

• Medicinal Chemistry
• Oncology
• Molecular Biology

Background:

• Microtubules, composed of alpha and beta-tubulin, are crucial for cell division, motility, and intracellular transport.
• Dysregulation of microtubule dynamics is implicated in various cancers, making them a key therapeutic target.
• Tubulin polymerization inhibitors have shown efficacy in cancer treatment, with several agents in development.

Purpose of the Study:

• To review important patents on tubulin polymerization inhibitors published between 2013 and 2018.
• To focus on tubulin inhibitors synthesized and studied in cancer research, detailing their structures and development phases.
• To highlight advancements in novel anticancer drug development targeting tubulin.

Main Methods:

• Patent literature review focusing on tubulin polymerization inhibitors from 2013-2018.
• Analysis of compound structures and their mechanisms of action.
• Assessment of preclinical and clinical development status of identified tubulin inhibitors.

Main Results:

• Approximately 20 patents were published between 2013 and 2018 concerning advanced cancer therapeutics targeting tubulin polymerization.
• Several tubulin inhibitors, including antibody-conjugated drugs (ACDs), are in various stages of drug development pipelines.
• Numerous heterocyclic compounds have demonstrated potent tubulin inhibitory activity and are under investigation for cancer therapy.

Conclusions:

• Targeting tubulin polymerization remains a promising strategy for developing novel anticancer drugs.
• Continued research into microtubule modulation is essential for discovering potent and effective cancer therapeutics.
• The development of new tubulin inhibitors, including those with heterocyclic scaffolds, offers significant potential for future cancer treatments.