| Synthesis of Some N-Alkoxycarbonyl-N″-benzoyl-benzamidrazones（p-toluamidrazones） and 1,3,5-Trisubstituted 1,2,4-Triazole Derivatives from N-Benzoylimidates and their Antimicrobial and Anticancer Screening Studies |
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| 作者姓名： | BEKIRCAN Olcay KAHVECI Bahittin OZGUMUS Osman Birol |
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| 作者单位： | [1]Department of Chemistry, Faculty of Arts and Sciences, Giresun University, 28049 Giresun, Turkey [2]Department of Chemistry, Faculty of Arts and Sciences, Rize University, 53100 Rize, Turkey [3]Department of Biology, Faculty of Arts and Sciences, Rize University, 53100 Rize, Turkey |
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| 基金项目： | Acknowledgements The authors thank the National Cancer Institute, USA, for the antitumor screening results. |
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| 摘 要： | Some new N-alkoxycarbonyl-N″-benzoyl-benzamidrazones （p-toluamidrazones） 3a-3d, and 1,3,5-trisubstituted 1,2,4-triazole 4a-4h derivatives by starting from N-benzoylbenzimidates or N-benzoyl-p-toluimidates. The structures of compounds 3 and 4 were established on the basis of elemental analyses, IR, ^1H NMR, ^13C NMR and UV data. Antimicrobial experiments of the compounds performed by using agar-well diffusion and broth microdilution methods revealed that only compounds 3a-3d, 4a and 4b showed inhibitory effect only on Candida albicans ATCC 60193. However, compound 4b had also specific antibacterial activity against Staphylococcus aureus ATCC 25923. The other compounds showed neither antifungal nor antibacterial activities. Compounds 3a, 4a and 4b have been screened on three human tumor cell lines, breast cancer （MCF7）, non small cell lung cancer （NCI-H460）, and CNS cancer （SF-268） at the National Cancer Institute （NCI）, USA, which were found to exhibit low antiproliferative activity.
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| 关 键 词： | 羰基 腙 1 2 4-三唑 抗癌效力 杀菌剂 |
| 收稿时间： | 2007-02-28 |
| 修稿时间： | 2007-05-11 |
Synthesis of Some N‐Alkoxycarbonyl‐N′′‐benzoyl‐benzamidrazones(p‐toluamidrazones) and 1,3,5‐Trisubstituted 1,2,4‐Triazole Derivatives from N‐Benzoylimidates and their Antimicrobial and Anticancer Screening Studies |
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| BEKIRCAN, Olcay KAHVECI, Bahittin OZGUMUS, Osman Birol.Synthesis of Some N‐Alkoxycarbonyl‐N′′‐benzoyl‐benzamidrazones(p‐toluamidrazones) and 1,3,5‐Trisubstituted 1,2,4‐Triazole Derivatives from N‐Benzoylimidates and their Antimicrobial and Anticancer Screening Studies[J].Chinese Journal of Chemistry,2007,25(12):1871-1877. |
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| Authors: | BEKIRCAN Olcay KAHVECI Bahittin OZGUMUS Osman Birol |
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| Institution: | 1. Fax: 0090‐454‐2164518;2. Department of Chemistry, Faculty of Arts and Sciences, Rize University, 53100 Rize, Turkey;3. Department of Biology, Faculty of Arts and Sciences, Rize University, 53100 Rize, Turkey |
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| Abstract: | Some new N‐alkoxycarbonyl‐N′′ ‐ benzoyl‐benzamidrazones (p‐toluamidrazones) 3a – 3d , and 1,3,5‐trisubstituted 1,2,4‐triazole 4a – 4h derivatives by starting from N‐benzoylbenzimidates or N‐benzoyl‐p‐toluimidates. The structures of compounds 3 and 4 were established on the basis of elemental analyses, IR, 1H NMR, 13C NMR and UV data. Antimicrobial experiments of the compounds performed by using agar‐well diffusion and broth microdilution methods revealed that only compounds 3a – 3d , 4a and 4b showed inhibitory effect only on Candida albicans ATCC 60193. However, compound 4b had also specific antibacterial activity against Staphylococcus aureus ATCC 25923. The other compounds showed neither antifungal nor antibacterial activities. Compounds 3a , 4a and 4b have been screened on three human tumor cell lines, breast cancer (MCF7), non small cell lung cancer (NCI‐H460), and CNS cancer (SF‐268) at the National Cancer Institute (NCI), USA, which were found to exhibit low antiproliferative activity. |
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| Keywords: | N-acylimidates carbonylhydrazone 1 2 4-triazoles anticancer activity antimicrobial activity |
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