Thiazolopyrimidine Scaffold as a Promising Nucleus for Developing Anticancer Drugs: A Review Conducted in Last Decade

The thiazolopyrimidine nucleus is a bioisosteric analog of purine and an important class of N-containing heterocycles. Thiazolopyrimidine scaffolds are considered a promising class of bioactive compounds that encompass diverse biological activities, such as antibacterial, antiviral, antifungal, anticancer, corticotrophin-releasing factor antagonists, anti-inflammatory, antituberculosis, and glutamic receptors antagonists. Despite the importance of thiazolopyrimidines from a pharmacological viewpoint, there is hardly a comprehensive review on this important heterocyclic nucleus. Throughout the years, those scaffolds have been studied extensively for its anticancer properties and several compounds were designed, synthesized, and evaluated for their anticancer effects with activity in the μM to nM range. However, there are hardly any reviews covering the anticancer effects of thiazolopyrimidines. In this review, an effort was made to compile literature covering the anticancer activity of thiazolopyrimidines reported in the last decade (2010-2020). Nearly thirty articles were reviewed and compounds with IC₅₀ < 50 μM against at least 50% of the used cell lines were listed in this review. The best ten compounds (10a, 14b, 17g, 18, 25e, 25k, 34e, 41i, 49a and 49c) showing the best anticancer activity against the corresponding cell lines during the last 10 years are highlighted. By highlighting the most active compounds, this review article sheds light on the structural features associated with the strongest anticancer effects to provide guidance for future research aiming to develop anticancer molecules.