- Synthesis and quantitative structure-activity relationship (QSAR) analysis of some novel oxadiazolo[3,4-d]pyrimidine nucleosides derivatives as antiviral agents
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We have synthesized a series of 4H,6H-[1,2,5]oxadiazolo[3,4-d]pyrimidine-5,7-dione 1-oxide nucleoside and their anti-vesicular stomatitis virus (VSV) activities in Wish cell were also investigated in vitro. It was found that most compounds showed obvious anti-VSV activities and compound 9 with ribofuranoside improved the anti-VSV activity by approximately 10 times and 18 times compared to didanosine (DDI) and acyclovir, respectively. A quantitative structure-activity relationship (QSAR) study of these compounds as well as previous reported oxadiazolo[3,4-d]pyrimidine nucleoside derivatives indicated that compounds with high activity should have small values of log P(o/w), vsurf-G and a large log S value. These findings and results provide a base for further investigations.
- Xu, Xiaojuan,Wang, Jun,Yao, Qizheng
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p. 241 - 244
(2015/02/19)
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- Convenient synthesis of toxoflavin that targets β-catenin/TCF4 signaling activities
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A rapid and improved route for synthesis of toxoflavin, an antibiotic and antitumor agent, is described. The method uses easily obtained materials and simple and practical reactions, including chlorination, condensation, and diazotization to produce toxoflavin in five steps with 14.2% yield and 98.6% purity (HPLC). This synthetic toxoflavin effectively inhibited β-catenin/Tcf4 driven TOP-luciferase activity with an IC50 of less than 0.5 μM and induced colon cancer cell death in a dose-dependent manner with an IC50 of 0.29 μM.
- Mao, Yongjun,Tian, Wang,Huang, Ziwei,An, Jing
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p. 594 - 597
(2014/06/10)
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- PURINES AND PYRIMIDINES AND CONDENSED SYSTEMS BASED ON THEM. 2. SYNTHESIS OF 1-METHYL-9-AMINOXANTHINE AND 9-AMINOTHEOPHYLLINE
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The previously unknown 9-aminotheophylline and 1-methyl-9-aminoxanthine were synthesized from 3-methyl-5-amino-6-hydrazinouracil.In the case of 1-methyl-9-aminoxanthine an x-ray diffraction study of an N-amino derivative of an NH heterocycle was made for the first time.
- Kuz'menko, V. V.,Kuz'menko, T. A.,Aleksandrov, G. G.,Pozharskii, A. F.,Gulevskaya, A. V.
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p. 690 - 697
(2007/10/02)
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