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Over the years, the branch of oncology has reached a mature stage, and substantial development and advancement have been achieved in this dimension of medical science. The synthesis and isolation of numerous novel anticancer agents of natural and synthetic origins have been reported. Thiazole and 4-thiazolidinone containing heterocyclic compounds, having a broad spectrum of pharmaceutical activities, represent a significant class of medicinal chemistry. Thiazole and 4-thiazolidinone are five-membered unique heterocyclic motifs containing S and N atoms as an essential core scaffold and have commendable medicinal significance. Thiazoles and 4-thiazolidinones containing heterocyclic compounds are used as building blocks for the next generation of pharmaceuticals. Thiazole precursors have been frequently used due to their capabilities to bind to numerous cancer-specific protein targets. Suitably, thiazole motifs have a biological suit via inhibition of different signaling pathways involved in cancer causes. The scientific community has always tried to synthesize novel thiazole-based heterocycles by carrying out different replacements of functional groups or skeleton around thiazole moiety. Herein, we report the current trend of research and development in anticancer activities of thiazoles and 4-thiazolidinones containing scaffolds. In the current study, we have also highlighted some other significant biological properties of thiazole, novel protocols of synthesis for the synthesis of the new candidates, along with a significant broad spectrum of the anticancer activities of thiazole containing scaffolds. This study facilitates the development of novel thiazole and 4-thiazolidinone containing candidates with potent, efficient anticancer activity and less cytotoxic property.
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