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The discovery of a series of combretastatin A-4 inspired novel molecular hybrids of 4-thiazolidinone-umbelliferones as prominent cytotoxic agents is reported. Representative compounds exhibited potent anti-proliferative activities against four human cancer...

Heterocycles closely intertwine chemistry with biology reflecting the presence of nitrogen‐based heterocyclic ring structure in nearly 75 % of small‐molecule drugs. The number of reported strategies for the synthesis of several “privileged scaffolds” has expanded, amongst which, cyclodesulfurization of thioureas offers a quick access to highly substituted heterocycles, thereby playing a role of an excellent tool in organic syntheses of natural products and pharmaceutically active compounds. This comprehensive review emphasizes the applications of cyclodesulfurization as an integral synthetic step in the synthesis of nitrogen, oxygen and sulfur‐containing heterocycles. Furthermore, a survey of cyclodesulfurizing agents reported since 2000 is comprehensively reviewed and summarized.

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