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Full-Text Articles in Physical Sciences and Mathematics
Preparation And Antimicrobial Activity Evaluation Of Some Quinoline Derivatives Containing An Azole Nucleus, Muhammet Özyanik, Serpi̇l Demi̇rci̇, Hakan Bektaş, Nesli̇han Demi̇rbaş, Ahmet Demi̇rbaş, Şengül Alpay Karaoğlu
Preparation And Antimicrobial Activity Evaluation Of Some Quinoline Derivatives Containing An Azole Nucleus, Muhammet Özyanik, Serpi̇l Demi̇rci̇, Hakan Bektaş, Nesli̇han Demi̇rbaş, Ahmet Demi̇rbaş, Şengül Alpay Karaoğlu
Turkish Journal of Chemistry
Quinoline-2-carbohydrazide (2) obtained from quinaldic acid (1) was converted to the corresponding carbothioamide 3 and carboxamide 6 by treatment with benzyliso(thio)cyanate. The basic treatment of 3 and 6 yielded the corresponding 1,2,4-triazole derivatives 4 and 7. The synthesis of 5-(quinolin-2-yl)-1,3,4- oxadiazol-2-thiol (9) was performed from the reaction of 1 with CS_2 in basic media. The Mannich reaction of compounds 4, 7, and 9 resulted in the formation of aminoalkylated derivatives 5a-c, 8, and 10a,b. The condensation of 1 with thiosemicarbazide, carbohydrazide, or thiocarbohydrazide gave the corresponding 1,2,4-triazole derivatives (11-13). The treatment of 4-amino-5-(quinolin-2-yl)- 4H-1,2,4-triazole-3-thiol (13) with 4-chlorophenacyl bromide caused the …
Design, Synthesis, And Biological Evaluation Of Indole-Based 1,4-Disubstituted Piperazines As Cytotoxic Agents, Meri̇ç Köksal Akkoç, Mi̇ne Yarim Yüksel, İrem Durmaz, Rengül Çeti̇n Atalay
Design, Synthesis, And Biological Evaluation Of Indole-Based 1,4-Disubstituted Piperazines As Cytotoxic Agents, Meri̇ç Köksal Akkoç, Mi̇ne Yarim Yüksel, İrem Durmaz, Rengül Çeti̇n Atalay
Turkish Journal of Chemistry
A series of 3-[(4-substitutedpiperazin-1-yl)methyl]-1H-indole derivatives were synthesized, and their structures were confirmed by spectral analysis. All the compounds were tested for their cytotoxic activity in vitro against 3 human tumor cell lines: human liver (HUH7), breast (MCF7), and colon (HCT116). Among the designed derivatives, most of the compounds showed significant cytotoxicity against liver and colon cancer cell lines with lower IC_{50} concentrations than the standard drug 5-fluorouracil. Compound 3s, with 3,4-dichlorophenyl substituent on the piperazine ring, was the most active in suppressing the growth of all screened cancer cells.
Synthesis And Cytotoxic Evaluation Of Uracil C-Mannich Bases, Hüseyi̇n İstanbullu, Istvan Zupko, Vi̇ldan Alptüzün, Erçi̇n Erci̇yas
Synthesis And Cytotoxic Evaluation Of Uracil C-Mannich Bases, Hüseyi̇n İstanbullu, Istvan Zupko, Vi̇ldan Alptüzün, Erçi̇n Erci̇yas
Turkish Journal of Chemistry
This study covers the design, synthesis, characterization, and cytotoxic activity of a series of uracil C-Mannich bases. Among them, one hybrid compound (1), a molecular combination of the potential antimetabolite substituted uracil and nitrogen mustard, having potential alkylating capability, was prepared as a Mannich base. The other compound was synthesized with the replacement of chlorines in the ethyl chains with hydroxyl groups for testing for anticancer activity. Some of Mannich bases having several amino groups with different pKa values were also synthesized and investigated in terms of cytotoxic activity. Their chemical structures were confirmed by means of their UV, IR, …