2. Academic Validation
  3. Novel thiazolidines: Synthesis, antiproliferative properties and 2D-QSAR studies

Novel thiazolidines: Synthesis, antiproliferative properties and 2D-QSAR studies

  • Bioorg Med Chem. 2019 Oct 15;27(20):115047. doi: 10.1016/j.bmc.2019.115047.
Ravi P Singh 1,  Marian N Aziz 2,  Delphine Gout 1,  Walid Fayad 3,  May A El-Manawaty 3,  Carl J Lovely 4
Affiliations

Affiliations

  • 1 Department of Chemistry and Biochemistry, University of Texas-Arlington, Arlington, TX 76019-0065, USA.
  • 2 Department of Chemistry and Biochemistry, University of Texas-Arlington, Arlington, TX 76019-0065, USA; Department of Pesticide Chemistry, National Research Centre, Dokki, Giza 12622, Egypt.
  • 3 Drug Bioassay-Cell Culture Laboratory, Pharmacognosy Department, National Research Centre, Dokki, Giza 12622, Egypt.
  • 4 Department of Chemistry and Biochemistry, University of Texas-Arlington, Arlington, TX 76019-0065, USA. Electronic address: lovely@uta.edu.
PMID: 31471102 DOI: 10.1016/j.bmc.2019.115047
Abstract

A series of N-substituted (Z)-2-imino-(5Z)-ylidene thiazolidines/thiazolidin-4-ones were synthesized and their antiproliferative activities against colon (HCT-116) and breast (MCF7) Cancer cell lines were evaluated utilizing an MTT growth assay. A 2D-QSAR investigation was conducted to probe and validate the obtained antiproliferative properties for the thiazolidine derivatives. The majority of the thiazolidines exhibit higher potency against a colon Cancer cell line relative to the standard reference. The p-halophenylimino p-anisylidene derivatives exhibited the highest anti-proliferative activity against HCT116 relative to control (IC50 = 8.9-10.0 μM compared to 20.4 μM observed for 5-fluorouracil as positive control). An X-ray study confirmed the Z, Z'-configurations for two examples of the synthesized compounds.

Keywords

2D-QSAR; HCT-116; One-pot; Tandem reaction.

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