Reference

Metabolic rate modification of nitrotriazole radiosensitizers by sulfur substitution of side chain

Metabolic rate modification of nitrotriazole radiosensitizers by sulfur substitution of side chain. Kagiya, V. Tsutomu; Sugita, Toshio; Nishimoto, Seiichi; Masuoka, Masamichi; Zhou, Lin; Abe, Mitsuyuki; Shibamoto, Yuta; Sasai, Keisuke (Kyoto Univ., Kyoto 606, Japan). Int. J. Radiat. Oncol., Biol., Phys., 22(3), 597-600 (English) 1992. CODEN: IOBPD3. ISSN: 0360-3016. DOCUMENT TYPE: Journal CA Section: 8 (Radiation Biochemistry) Section cross-reference(s): 14 The pharmacokinetic properties and radiosensitizing activities in vitro and in vivo of a series of 3-nitro-1,2,4-triazole (NTA) derivs. with a -CH2(C = Y)NH(CH2)nZCH3 (Y, Z = O or S; n = 2 or 3) group in the side chain at N-1 position of NTA were investigated with respect, particularly, to the effects of sulfur substitution in the side chain of NTA. The sulfur substitution for an oxygen atom in the side chain NTA radiosensitizers increased the p value, but gave rise to little effect on the one-electron redn. 24807-55-4 is also in the experiment. potential. The derivs. bearing a thioether group (-CH2SCH3) in the side chain were slightly less effective both in vitro on hypoxic EMT6/KU cells and in vivo on SCCVII tumors than their oxygen analogs (-CH2OCH3). The thioether compds. tended to metabolize rapidly. The thioamide compd. showed high sensitizing activity in vitro, but metabolized very slowly. .

Highly effective phosphotriester method for oligodeoxyribonucleotide synthesis

Highly effective phosphotriester method for oligodeoxyribonucleotide synthesis. Azole-anion catalysis in the presence of crown ethers. Sinyakov, A. N.; Lebedev, A. V. (All-Union Res. Inst. Mol. Biol., Koltsovo, USSR). Bioorg. Khim. 17455-13-9 and 24807-55-4 which are cas registry numbers are also used here., 12(8), 1129-31 (Russian) 1986. CODEN: BIKHD7. DOCUMENT TYPE: Journal CA Section: 33 (Carbohydrates) K salts of tetrazole or 3-nitro-1,2,4-triazole in the presence of equimol. amts. of 18-crown-6 are effective nucleophilic catalysts for the phosphotriester synthesis of oligodeoxyribonucleotides. 31P-NMR data demonstrated that phosphotriazolides (tetrazolides) are the intermediates in the reaction of phosphotriester condensation. K 3-nitro-1,2,4-triazolide - 18-crown-6 was used for prepn. of two decanucleotides, e.g., (T)10 and ATGGTTTTTC, in high yield (92-93.5% per coupling cycle). .