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Rohidas M. Jagtap¹, Sachin S. Sakate¹, Satish K. Pardeshi² and Masood A. Rizvi³¹Department of Chemistry, P. E. S. Modern College of Arts, Science and Commerce (Autonomous), Shivajinagar, Pune, MS, India²Department of Chemistry, Savitribai Phule Pune University (Formerly University of Pune), Ganeshkhind, Pune, MS, India³Department of Chemistry, University of Kashmir, Hazratbal, Srinagar, Jammu and Kashmir, IndiaPart of the book: Advances in Chemistry Research. Volume 76Chapter DOI: https://doi.org/10.52305/KSNB2027AbstractThe X-ray crystallography is credibly an unequivocal state of art tool for authentication of the stereochemistry of chiral bioactive organic compounds. The acquired diffraction data processed to deliver the exact stereostructure of the compound which can be further correlated to the biological activity of that compound. The 2-alkyl/aryl thiazolidine-4- carboxylic acids (2A-T4CA) and their derivatives have sufficient H-bonding sites which enables the researcher to crystallize them to an absolute purity for diffraction by single crystal X-ray spectroscopy. In this regard, the thiazolidine class of organosulfur compounds and some of their organometallic complexes have been explored by the researchers for their single crystal X-ray structures. Apart from the cardiovascular diseases, cancer stands second in human mortality. The discovery and development of small molecular drugs (SMD) for cancer treatment is always desired as they are more effective in genetic additions, dependencies and vulnerabilities of cancer cells. Considering the SMD application of T4CA and their derivatives, these thioazolidines are widely investigated by various research groups for their in vitro anticancer activities against several human cancer cell lines. 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