- Synthesis and cytotoxic activity study of novel 2-(Aryldiazenyl)-3-methyl-1h-benzo[g]indole derivatives
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A novel series of 2-(aryldiazenyl)-3-methyl-1H-benzo[g]indole derivatives (3a–f) were prepared through the cyclization of the corresponding arylamidrazones, employing polyphosphoric acid (PPA) as a cyclizing agent. All of the compounds (3a–f) were characterized using1H NMR,13C NMR, MS, elemental analysis, and melting point techniques. The synthesized compounds were evaluated for cytotoxic activity against diverse human cancer cell lines by the National Cancer Institute. While all of the screened compounds were found to be cytotoxic at a 10 μM concentration, two of them (2c) and (3c) were subjected to five dose screens and showed a significant cytotoxicity and selectivity.
- Abdel-Jalil, Raid J.,Adham, Sirin A. I.,Arafeh, Manar M.,Moghadam, Ebrahim Saeedian,Stoll, Raphael
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- Design and synthesis of pyrazolo[3,4-d]pyridazine 5,6-dioxides as novel NO-donors
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A simple and effective protocol for the synthesis of 2H-pyrazolo[3,4-d]pyridazine 5,6-dioxides includes a transformation of accessible 3,4-diacetyl-5-methyl-1H-pyrazoles into the corresponding 1,4-dioximes followed by their N2O4- mediated oxidative cyclization. All transformations proceed under mild conditions in good to high yields. According to the Griess assay, synthesized 2H-pyrazolo[3,4-d]pyridazine 5,6-dioxides showed promising NO-donor profiles producing NO in a wide range of concentrations.
- Kulikov, Alexander S.,Epishina, Margarita A.,Zhilin, Egor S.,Shuvaev, Alexander D.,Fershtat, Leonid L.,Makhova, Nina N.
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- Application of phenylhydrazine base ketone compound as agricultural bactericide
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The invention relates to an application of phenylhydrazine base ketone compound as agricultural bactericide, the application of the phenylhydrazine base ketone compound disclosed in a formula (1) for inhibiting or killing fungi which cause crop diseases and the application of the phenylhydrazine base ketone compound as the agricultural bactericide. The phenylhydrazine base ketone compound has the advantage of high activity when being used for inhibiting the fungi which cause crop diseases to grow, is suitable for preventing and curing plant diseases caused by the fungi and can be used for preventing and curing diseases caused by various fungi including rice blast and wheat scab, wherein R1, R2, R3, R4 and R5 are respectively independently selected from hydrogen, halogen, alkyl group, alkoxy, hydroxyl, cyanogroup, trifluoromethyl, sulfamide and nitryl; R6 is selected from hydrogen, halogen, alkyl group, amino, cyanogroup, CH3CH2S-, CH3CO-, CF3CH2CO- or CF3CO- and the like; R7 is alkyl group, hydroxyl, phenyl, halogenated phenyl, alkoxy and trifluoromethyl; X can be nitrogen or carbon, and R5 is not in the presence when X is nitrogen, the formula (1) is shown in the description.
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Paragraph 0088-0090; 0092
(2017/12/13)
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- HETEROCYCLES FROM NITRILE IMINES. PART IV. CHIRAL 4,5-DIHYDRO-1,2,4-TRIAZIN-6-ONES
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The reaction of nitrile imines (II) with α-amino esters (III) proceeds with no detectable racemization and constitutes a convenient synthetic route to 4,5-dihydro-1,2,4-triazin-6-ones (IV).Permangamate oxidation of heterocycles (IV) affords the corresponding 1,2,4-triazin-6-ones (V).The reaction of (II) with β-amino esters gives the respective acyclic amidrazone adducts (VI).
- El-Abadelah, Mustafa M.,Hussein, Ahmad Q.,Thaher, Bassam A.
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p. 1879 - 1895
(2007/10/02)
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