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首页> 外文期刊>Inorganica Chimica Acta >Phosphorus nitrogen compounds: Part 34. Syntheses, structural investigations, cytotoxic and biological activities of spiro-ansa-spiro and spiro-bino-spiro tetrameric phosphazene derivatives
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Phosphorus nitrogen compounds: Part 34. Syntheses, structural investigations, cytotoxic and biological activities of spiro-ansa-spiro and spiro-bino-spiro tetrameric phosphazene derivatives

机译:磷氮化合物:第34部分。螺-螺-螺-螺和螺-螺-螺-螺四聚磷腈衍生物的合成,结构研究,细胞毒性和生物学活性

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The reactions of N4P4Cl8 with the symmetric N2N2 (1-3) and N2O2 (4) bulky ligands gave partly substituted 2,4-sas (5 and 6), 2,6-sas (7-10) and sbs (11-14) tetrameric phosphazene derivatives. The 2,4-sas-5, 2,6-sas-8 and sbs-12 reacted with pyrrolidine to give fully-substituted tetra-(15 and 16) and dode-capyrrolidinocyclotetraphosphazenes (17-19). The structures of all the phosphazenes were verified by FTIR, MS, H-1, C-13{H-1} and P-31{H-1} NMR, and HSQC spectral data. The crystal structures of 7, 9 and 10 were examined by single crystal X-ray diffraction techniques. The compounds 1-3, 5, 8, 9, 12, 13, 16 and 18 were screened for antimicrobial activity against G(+) and G(-) bacteria and fungi. The compound 16 is found to possess excellent activity (MIC values of 39 and 78 mu M) against fungal pathogen Candida krusei and Candida albicans. Meanwhile, interactions between pBR322 plasmid DNA and 1-3, 5, 8, 9, 12, 13, 14, 16 and 18 were investigated by agarose gel electrophoresis. The compounds 5, 8, 9, 12, 13, 16 and 18 were appraised for their cytotoxic activity against L929 Fibroblast and MDA-MB-231 breast cancer cell lines. Compounds 13 and 16 are as effective as cis-platin. (C) 2016 Elsevier B.V. All rights reserved.
机译:N4P4Cl8与对称的N2N2(1-3)和N2O2(4)庞大的配体反应生成部分取代的2,4-sas(5和6),2,6-sas(7-10)和sbs(11-14) )四聚磷腈衍生物。 2,4-sas-5、2,6-sas-8和sbs-12与吡咯烷反应,得到完全取代的四-(15和16)和十二烷基-吡咯烷基环四磷腈(17-19)。通过FTIR,MS,H-1,C-13 {H-1}和P-31 {H-1} NMR和HSQC光谱数据验证了所有磷腈的结构。通过单晶X射线衍射技术检查了7、9和10的晶体结构。筛选化合物1-3、5、8、9、12、13、16和18的抗G(+)和G(-)细菌和真菌的抗菌活性。发现化合物16具有对抗真菌病原体假丝酵母和白色念珠菌的优异活性(MIC值为39和78μM)。同时,通过琼脂糖凝胶电泳研究pBR322质粒DNA与1-3、5、8、9、12、13、14、16和18之间的相互作用。评估化合物5、8、9、12、13、16和18对L929成纤维细胞和MDA-MB-231乳腺癌细胞系的细胞毒活性。化合物13和16与顺铂一样有效。 (C)2016 Elsevier B.V.保留所有权利。

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