2. Academic Validation
  3. Synthesis, biological evaluation and molecular modeling studies of some novel thiazolidinediones with triazole ring

Synthesis, biological evaluation and molecular modeling studies of some novel thiazolidinediones with triazole ring

  • Eur J Med Chem. 2013:70:308-14. doi: 10.1016/j.ejmech.2013.10.005.
Yakaiah Chinthala 1,  Anand Kumar Domatti,  Alam Sarfaraz,  Shailendra Pratap Singh,  Niranjan Kumar Arigari,  Namita Gupta,  Srinivas K V N Satya,  Jonnala Kotesh Kumar,  Feroz Khan,  Ashok K Tiwari,  Grover Paramjit
Affiliations

Affiliation

  • 1 Natural Product Chemistry, CSIR-Central Institute of Medicinal and Aromatic Plants-Research Centre, Boduppal, Hyderabad 500092, A.P., India.
PMID: 24177357 DOI: 10.1016/j.ejmech.2013.10.005
Abstract

A new series of thiazolidinedione derivatives were synthesized and evaluated for in vitro α-glucosidase inhibition and Anticancer activities. Compounds 3d, 3e and 3j showed potential α-glucosidase inhibition with IC₅₀ values ranging between 0.1 and 0.3 μg/ml whereas compounds 3i, 3j and 3k have showed better Anticancer activity towards human Cancer cell lines IMR-32 (neuroblastoma), Hep-G2 (hepatoma) and MCF-7 (breast). Molecular docking studies revealed compounds 3d, 3e and 3j are potent inhibitors of α-glucosidase and also showed compliance with standard parameters of drug likeness.

Keywords

1,2,3-Triazoles; Anticancer activity; Molecular modeling study; Thiazolidinediones; α-Glucosidase inhibition.

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