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
  • 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.