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Title Synthesis, Antibacterial and Anticancer Activities Evaluation of New 4-Thiazolidinone-Indolin-2-One Analogs
Type JournalPaper
Keywords isatin; thiazolidinone; isatin-thiazolidinone hybrids; apoptosis; cancer cells
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
Researchers Alireza Foroumadi (Not In First Six Researchers), Fatemeh Safari (Not In First Six Researchers), reza Nezamdoost Darestani (Fifth Researcher), Marjan Azimzadeh Arani (Fourth Researcher), Mahdieh Darroudi (Third Researcher), Yaghoub Sarrafi (Second Researcher), Mahshid Hamzehloueian (First Researcher)