- Synthesis, biological evaluation and molecular docking studies of 3-(1,3-diphenyl-1H-pyrazol-4-yl)-N-phenylacrylamide derivatives as inhibitors of HDAC activity
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In present study, a series of 3-(1,3-diphenyl-1H-pyrazol-4-yl)-N- phenylacrylamide derivatives (5a-8d) were designed, synthesized, and evaluated for HDAC inhibition and tumor cell antiproliferation. All of these compounds are reported for the first time,
- Li, Xi,Liu, Jia-Lin,Yang, Xian-Hui,Lu, Xiang,Zhao, Ting-Ting,Gong, Hai-Bin,Zhu, Hai-Liang
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p. 4430 - 4436
(2012/08/29)
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- Microwave-Assisted Synthesis of 3-(4-Pyrazolyl)propenoic Acids
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Under microwave activation, pyrazole-4-carboxaldehydes react with malonic acid in the presence of a small amount of pyridine to give 3-(4-pyrazolyl)propenoic acids in high yields.
- Chornous, Vitaliy O.,Bratenko, Mykhaylo K.,Vovk, Mykhaylo V.
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- Functionally substituted 3-heterylpyrazoles: XI. 3-[3-Aryl(heteryl)pyrazol-4-yl]propenoic and propanoic acids
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3-Aryl(heteryl)-4-formylpyrazoles by condensation with malonic acid furnish 3-[3-aryl(heteryl)-pyrazol-4-yl]propenoic acids that in the presence of Raney nickel are reduced by hydrazine hydrate to 3-[3-aryl(heteryl)pyrazol-4-yl]propanoic acids. The succes
- Bratenko,Chornous,Vovk
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p. 1171 - 1177
(2007/10/03)
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- Azoles. 17. Beta-(4-pyrazol)acrylic and propionic acids and their anti-inflammatory activity
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beta-(4-Pyrazole)acrylic acids 22-28 were prepared by the Knoevenagel reaction of malonic acid and 4-formylpyrazoles 8-14. 4-Pyrazolemethylenemalonic acids 15-21 were isolated as intermediates. The latter compounds were also synthesized by treating the 4-formylpyrazoles 8-14 with diethyl malonate followed by hydrolysis of the obtained diethyl esters 15a-21a. The effect of piperidine and pyridine on the Knoevenagel condensation was investigated. The beta-(4-pyrazole)acrylic acids 22-27, on catalytic reduction, gave the corresponding beta-(4-pyrazole)propionic acids 29-34. Compounds 23, 24, 27, 29-31 and 34 appeared to be less active than phenylbutazone in carrageenin-induced oedema test, but they were less toxic than the reference drug.
- Bernard,Hulley,Molenda,Stochla,Wrzeciono
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p. 560 - 562
(2007/10/02)
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