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

[Display omitted] 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 conducte...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2019-10, Vol.27 (20), p.115047-115047, Article 115047
Main Authors: Singh, Ravi P., Aziz, Marian N., Gout, Delphine, Fayad, Walid, El-Manawaty, May A., Lovely, Carl J.
Format: Article
Language:English
Subjects:
2D-QSAR
HCT-116
One-pot
Tandem reaction
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Summary:[Display omitted] 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.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2019.115047