Twenty years of quinazolines as tubulin polymerisation inhibitors

Over the past two decades, the quinazoline scaffold has emerged as a privileged framework in the development of small-molecule tubulin polymerisation inhibitors. Here we map the chemical space of these compounds and outline the key structure-activity relationships that define this class. In line with recent recognition of the value of polypharmacology in cancer treatment, we compiled quinazoline structures and associated biological data on tubulin polymerisation, growth inhibition, and anticancer potential from SciFinder, PubMed, and the ChEMBL database. Studies lacking direct evidence of tubulin engagement are noted only briefly. Relevant work on quinones and C-to-N isosteric quinazoline analogues is also summarised where appropriate.