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Synthesis, Antibacterial and Anticancer Activities Evaluation of New 4-Thiazolidinone-Indolin-2-One Analogs Publisher



Hamzehloueian M1 ; Sarrafi Y2 ; Darroudi M2, 3 ; Arani MA4 ; Darestani RN5 ; Safari F5 ; Foroumadi A4, 6
Authors
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Authors Affiliations
  1. 1. Department of Chemistry, Jouybar Branch, Islamic Azad University, Jouybar, Iran
  2. 2. Department of Organic Chemistry, Faculty of Chemistry, University of Mazandaran, Babolsar, Iran
  3. 3. Department of Physiology, Faculty of Medicine, Mashhad University of Medical Science, Mashhad, Iran
  4. 4. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
  5. 5. Department of Biology, Faculty of Science, University of Guilan, Rasht, Iran
  6. 6. Drug Design and Development Research Center, The Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medical Sciences, Tehran, Iran

Source: Biointerface Research in Applied Chemistry Published:2022


Abstract

A series of novel thiazolidinone-isatin hybrids have been synthesized through the Knoevenagel reaction of isatin derivatives with synthesized thiazolidinone scaffolds and then evaluated for their in vitro antibacterial effects on Escherichia coli (E.coli) and Staphylococcus aureus (S.aureus). Cytotoxic effects of the compounds on non-small-cell lung cancer cells (A549 cells), breast epithelial cancer cell line (MCF-7), and prostate cancer cells (PC3 cells) were investigated. Among compounds tested for antibacterial activity, S. aureus was susceptible to compound 7d. The most potent compounds against A549, MCF-7, and PC3 tumor cells were found to be 7g. DAPI staining of all cancer cell lines treated with compound 7g, associated with cell death. We finally confirmed that apoptosis occurred in A549 cells by up-regulated Bax expression and down-regulated Bcl-2 expression from the mitochondrial pathway of apoptosis by using the quantitative reverse transcription-polymerase chain reaction (qRT-PCR) method. Our findings suggested that compound 7g may be a good target in designing cancer therapy strategies. © 2021 by the authors.