Novel thiazolidines: Synthesis,antiproliferative properties and 2D-QSAR studies |
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| Affiliation: | 1. Department of Chemistry and Biochemistry, University of Texas-Arlington, Arlington, TX 76019-0065, USA;2. 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;1. Department of Pharmaceutical Chemistry, ISF College of Pharmacy, Moga 142001, Punjab, India;2. Department of Pharmacology, ISF College of Pharmacy, Moga 142001, Punjab, India;1. Department of Organic and Bioorganic Chemistry, Faculty of Pharmacy in Hradec Králové, Charles University, Akademika Heyrovského 1203, 500 05 Hradec Králové, Czech Republic;2. Department of Biological and Biochemical Sciences, Faculty of Chemical Technology, University of Pardubice, Studentská 573, 532 10 Pardubice, Czech Republic;1. Chemistry Department, Faculty of Science, Ain Shams University, Cairo, Egypt;2. Department of Chemistry & Physics, Augusta University, Augusta, GA 30912, USA;3. Pesticide Chemistry Department, National Research Centre, Dokki, Giza 12622, Egypt;4. X-ray Crystallography Laboratory, Physics Division, National Research Centre, Dokki, Giza 12622, Egypt;1. Research Institute for Fundamental Sciences (RIFS), University of Tabriz, Tabriz, Iran;2. Department of Medical Biotechnology, Faculty of Advanced Medical Sciences, Tabriz University of Medical Sciences, Tabriz, Iran |
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| 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. |
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| Keywords: | One-pot Tandem reaction HCT-116 2D-QSAR |
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