Advancements of Emerging Thiazole‐Based CDKs Inhibitors for Cancer Therapy: From Hits to Clinical Candidates

ABSTRACT Cyclin‐dependent kinases (CDKs) represent highly attractive anticancer targets and several inhibitors have been approved for cancer therapy. However, drug resistance and dose‐dependent toxicity have limited clinical application. Therefore, discovering new CDKs inhibitors featuring novel scaffolds and high selectivity for disease treatment and target research remains to attract significant interest from both academics and industry. Recently, thiazole has emerged as a privileged heterocyclic scaffold for design and synthesis of antitumor drugs targeting CDKs. Currently, although there are no FDA‐approved thiazole‐based CDKs inhibitors, this review systematically summarizes the evolution of inhibitors from early hits to clinical‐stage candidates including GFH009, SNS‐032, and JSH‐150, with particular emphasis on structure‐based drug design strategies. Furthermore, we highlight the challenges and future prospects in development of thiazole derivatives targeting CDKs, with particular emphasis on discovery of next‐generation, highly selective inhibitors.