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ANTICANCER POTENTIAL OF COMPOUNDS BEARING THIAZOLIDIN-4-ONE SCAFFOLD: COMPREHENSIVE REVIEW
被引:4
|作者:
Singh, Dalbir
[1
]
Piplani, Mona
[1
]
Kharkwal, Harsha
[2
]
Murugesan, Sankaranarayanan
[3
]
Singh, Yogendra
[1
]
Aggarwal, Amit
[1
]
Chander, Subhash
[2
]
机构:
[1] Maharaja Agrasen Univ, Sch Pharm, Solan 174103, Himachal Prades, India
[2] Amity Univ Uttar Pradesh, Amity Inst Phytochem & Phytomed, Noida 201313, India
[3] Birla Inst Technol & Sci Pilani, Dept Pharm, Med Chem Res Lab, Pilani Campus, Pilani 333031, Rajasthan, India
来源:
关键词:
Thiazolidin-4-one;
Cytotoxicity;
Drug discovery;
Selectivity;
Anti-cancer;
Structure-activity relationship (SAR);
ARYLAMINE N-ACETYLTRANSFERASES;
IN-VITRO;
SUBSTITUTED THIAZOLIDIN-4-ONES;
THIAZOLIDINE-4-ONE DERIVATIVES;
BIOLOGICAL EVALUATION;
MOLECULAR DOCKING;
BREAST-CANCER;
KAPPA-B;
4-THIAZOLIDINONE;
DESIGN;
D O I:
10.51847/oHzuia1yg6
中图分类号:
R9 [药学];
学科分类号:
1007 ;
摘要:
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.
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页码:56 / 70
页数:15
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