Journal
MEDICINAL RESEARCH REVIEWS
Volume 42, Issue 1, Pages 513-575Publisher
WILEY
DOI: 10.1002/med.21852
Keywords
anticancer; DNA intercalation; structure-activity relationship; sulfur heterocycles; tubulin inhibition
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Funding
- DoP, the Ministry of Chemicals & Fertilizers, Govt. of India, New Delhi
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This review provides a comprehensive report on the design strategies of sulfur-bearing cytotoxic agents and their potential in anticancer therapy. The article discusses various sulfur-containing heterocyclic scaffolds and their cytotoxic effects through multiple mechanisms. The assessment of antiproliferative activities allows for a proficient evaluation of the structure-activity relationships of the synthesized molecules.
This review article proposes a comprehensive report of the design strategies engaged in the development of various sulfur-bearing cytotoxic agents. The outcomes of various studies depict that the sulfur heterocyclic framework is a fundamental structure in diverse synthetic analogs representing a myriad scope of therapeutic activities. A number of five-, six- and seven-membered sulfur-containing heterocyclic scaffolds, such as thiazoles, thiadiazoles, thiazolidinediones, thiophenes, thiopyrans, benzothiazoles, benzothiophenes, thienopyrimidines, simple and modified phenothiazines, and thiazepines have been discussed. The subsequent studies of the derivatives unveiled their cytotoxic effects through multiple mechanisms (viz. inhibition of tyrosine kinases, topoisomerase I and II, tubulin, COX, DNA synthesis, and PI3K/Akt and Raf/MEK/ERK signaling pathways), and several others. Thus, our concise illustration explains the design strategy and anticancer potential of these five- and six-membered sulfur-containing heterocyclic molecules along with a brief outline on seven-membered sulfur heterocycles. The thorough assessment of antiproliferative activities with the reference drug allows a proficient assessment of the structure-activity relationships (SARs) of the diversely synthesized molecules of the series.
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