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TÜBİTAK

Turkish Journal of Chemistry

2017

Cytotoxicity

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Synthesis And Cytotoxicity Of Novel Thioxo-Quinazolino[3,4-$A$]Quinazolinones, Negar Mohammadhosseini, Mina Saeedi, Shahram Moradi, Mohammad Mahdavi, Omidreza Firuzi, Alireza Foroumadi, Abbas Shafiee Jan 2017

Synthesis And Cytotoxicity Of Novel Thioxo-Quinazolino[3,4-$A$]Quinazolinones, Negar Mohammadhosseini, Mina Saeedi, Shahram Moradi, Mohammad Mahdavi, Omidreza Firuzi, Alireza Foroumadi, Abbas Shafiee

Turkish Journal of Chemistry

Various thioxo-quinazolino[3,4-$a$]quinazolinones were prepared and evaluated for their cytotoxicity in MOLT-4 (lymphoblastic leukemia) and MCF-7 (breast adenocarcinoma) cell lines. Synthesis of the target compounds was started from isatoic anhydride. Successive reaction of isatoic anhydride with benzylamine and 2-nitrobenzaldehyde, reduction of the nitro group, and reaction with CS$_{2}$ gave 12-benzyl-6-thioxo-6,7,11b,12-tetrahydro-13$H$-quinazolino[3,4-$a$]quinazolin-13-one. The latter compound reacted with various 2-chloro-$N$-substituted acetamides to afford the corresponding fused quinazolinone derivatives.


Synthesis And Anticancer And Cytotoxic Effects Of Novel 1,4-Phenylene-Bis-N-Thiocarbamoylpyrazole And 1,4-Phenylene-Bis-Pyrazolylthiazole Derivatives, Meli̇ha Burcu Gürdere, Erdoğan Kamo, Yakup Budak, Ayşe Şahi̇n Yağlioğlu, Mustafa Ceylan Jan 2017

Synthesis And Anticancer And Cytotoxic Effects Of Novel 1,4-Phenylene-Bis-N-Thiocarbamoylpyrazole And 1,4-Phenylene-Bis-Pyrazolylthiazole Derivatives, Meli̇ha Burcu Gürdere, Erdoğan Kamo, Yakup Budak, Ayşe Şahi̇n Yağlioğlu, Mustafa Ceylan

Turkish Journal of Chemistry

Thiazolylpyrazoline derivatives were recently reported as potent anticancer agents. In this study, novel 1,4-phenylene-bis-N-thiocarbamoylpyrazoles (3a-h and 1,4-phenylene-bis-pyrazolylthiazoles (5a-h were prepared and screened for their anticancer activities against C6 (rat brain tumor cells) and HeLa (human uterus carcinoma). Anticancer activity studies were performed as a dose-dependent assay starting with eight concentrations. 5-Fluorouracil (5-FU) was used as a positive control. Compounds 3c, 3d, and 3h were examined and they revealed almost the same activities compared with 5-FU in terms of cell selectivity against C6 cells. Moreover, compounds 3a-h had lower cytotoxicity than 5-FU. The low cytotoxicity values of 3a-h as well as …