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    Phosphorus-nitrogen compounds Part 32. Structural and thermal characterizations, antimicrobial and cytotoxic activities, and in vitro DNA binding of the phosphazenium salts
    (Springer, 2016) Akbas, Huseyin; Okumus, Aytug; Karadag, Ahmet; Kilic, Zeynel; Hokelek, Tuncer; Koc, L. Yasemin; Turk, Mustafa
    The salicylic acid salts of fully substituted mono(4-fluorobenzyl)spirocyclotriphosphazenes (10-15) were prepared. The structures of these phosphazenium salts (10a-15a) were determined by elemental analyses, FTIR and H-1, C-13{H-1}, P-31{H-1} NMR techniques. The crystal structure of 14a was verified by X-ray diffraction analysis. The thermal properties of the salts were investigated using TG/DTA and DSC instruments. The results obtained from DSC indicated that the melting temperatures and latent heats of the compounds were in the ranges of 107.76-143.04 A degrees C and 41.64-69.73 J g(-1), respectively. The thermal stabilities of the phosphazenium salts (10a-15a) are found to be different, but they have a similar decomposition mechanism. The compounds 14a and 15a exhibit noticeable cytotoxic activity against DLD-1 cancer cells, and they seem to be good candidates for being anticancer agents. All of the compounds have an antimicrobial effect on bacterial and yeast strains within the ranges of 312-625 A mu M (bacterial strains) and 19.5-312 A mu M (yeast strains). It is found that compounds 13a-15a were most effective against yeast strains. Moreover, interactions between the salts and pBR322 plasmid DNA show that 14a and 15a cleave the DNA and decrease the intensity of form I. BamHI and HindIII digestion results demonstrate that the compounds are not bound with G/G and A/A nucleotides, respectively.
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    Phosphorus-nitrogen compounds part 33: in vitro cytotoxic and antimicrobial activities, DNA interactions, syntheses, and structural investigations of new mono(4-nitrobenzyl)spirocyclotriphosphazenes
    (Springer, 2016) Okumus, Aytug; Akbas, Huseyin; Kilic, Zeynel; Koc, L. Yasemin; Acik, Leyla; Aydin, Betul; Dal, Hakan
    The condensation reactions of hexachlorocyclotriphosphazene, N3P3Cl6, with N-alkyl-N'-mono(4-nitrobenzyl)diamines (1-3), NO2PhCH2NH(CH2) (n) NHR1 (R-1 = CH3 or C2H5), led to the formation of the mono(4-nitrobenzyl)spirocyclotriphosphazenes (4-6). The tetra-pyrrolidino (4a-6a), piperidino (4b-6b), and 1,4-dioxa-8-azaspiro[4,5]decaphosphazenes (4c-6c) were prepared from(for) the reactions of partly substituted compounds (4, 5, and 6) with excess pyrrolidine, piperidine, and 1,4-dioxa-8-azaspiro[4,5]decane (DASD), respectively. The partly substituted geminal (4d and 5d) and cis-morpholino (6d) phosphazenes were isolated from the reactions of excess morpholine in boiling THF and o-xylene, but the expected fully substituted compounds were not obtained. The structures of all the phosphazene derivatives were determined by elemental analyses, MS, FTIR, H-1, C-13{H-1}, P-31{H-1} NMR, HSQC, and HMBC techniques. The crystal structures of 4, 6, 4a, and 5a were verified by X-ray diffraction analysis. In addition, in vitro cytotoxic activities of fully substituted phosphazenes (4a-6c) against HeLa cervical cancer cell lines (ATCC CCL-2) and the compounds 4a and 4c against breast cancer cell lines (MDA-MB-231) and L929 fibroblast cells were evaluated, respectively. Apoptosis effect was determined by MDA-MB-231 cancer cell lines and fibroblast cells. The MIC values of the compounds were in the ranges of 9.8-19.5 A mu M. The compounds 6, 5a, 6a, 5b, and 6d have greater MIC activity against bacterial and yeast strain. The investigation of DNA binding with the phosphazenes was studied using plasmid DNA. The phosphazene derivatives inhibit the restriction endonuclease cleavage of plasmid DNA by BamHI and HindIII enzymes. BamHI and HindIII digestion results demonstrate that the compounds bind with G/G and A/A nucleotides.