TY  - JOUR
T1  - Anticancer Potential of Compounds Bearing Thiazolidin-4-one Scaffold: Comprehensive Review
A1  - Dalbir Singh
A1  - Mona Piplani
A1  - Harsha Kharkwal
A1  - Sankaranarayanan Murugesan
A1  - Yogendra Singh
A1  - Amit Aggarwal
A1  - Subhash Chander
JF  - Pharmacophore
JO  - Pharmacophore
SN  - 2229-5402
Y1  - 2023
VL  - 14
IS  - 1
DO  - 10.51847/oHzuia1yg6
SP  - 56
EP  - 70
N2  - Thiazolidin-4-ones is a versatile and privileged nucleus comprising of a five five-membered heterocyclic ring system possessing sulphur heteroatom and a cyclic amide bond. Extensive research and review studies mainly published in the last decade explored the diverse types of biological activities of this nucleus with potential therapeutic applications. Various silent features like drug likeness behaviour, suitability for diversity-oriented synthesis, and its sensitivity toward the redox tumour microenvironment makes it an attractive scaffold for anti-cancer drug discovery. Thiazolidine-2,4-dione and thiazolidine-4-ones are the two classical variants of thiazolidine scaffold, the former is more explored in comparison to thiazolidine-4-one. However, thiazolidine-4-one nucleus is also getting the attention of researchers, evident by the various research studies, mainly published in the last few years.

The current comprehensive review focuses on its anti-cancer potential, covering structural diversity and substitution patterns among diverse derivatives containing this nucleus as a core skeleton. This review also gives impetus to the different enzymatic targets, exploited for drug discovery, relative selectivity in cancerous tissue compared to healthy counterpart cells, structure-activity relationship (SAR), and future perspectives for translational research. To generate potential lead candidates with the translational outcome next level studies like pharmacokinetic and metabolic stability are suggested.
UR  - https://pharmacophorejournal.com/article/anticancer-potential-of-compounds-bearing-thiazolidin-4-one-scaffold-comprehensive-review-xtncwjhzxhicwgh
ER  -