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Design, Synthesis and Biological Activities of New Pyrazole Derivatives Possessing Both Coxib and Combretastatins Pharmacophores
Chemistry and Biodiversity Số 6, năm 2019 (Tập 16, trang -)
DOI: 10.1002/cbdv.201900108
Tài liệu thuộc danh mục: Scopus
English
Từ khóa: 4 [3 (trifluoromethyl) 5 (3,4,5 trimethoxyphenyl) 1h pyrazol 1 yl]benzenesulfonamide; celecoxib; combretastatin A4; cyclooxygenase 2 inhibitor; cytotoxic agent; ellipticine; ethyl 1 (4 cyanophenyl) 4,5 diphenyl 1h pyrazole 3 carboxylate; ethyl 1 (4 methoxyphenyl) 4,5 diphenyl 1h pyrazole 3 carboxylate; ethyl 1 (4 nitrophenyl) 4,5 diphenyl 1h pyrazole 3 carboxylate; ethyl 1(4 cyanophenyl) 4,5 bis(4 methoxyphenyl) 1h pyrazole 3 carboxylate; ethyl 1,4,5 tris(4 methoxyphenyl) 1h pyrazole 3 carboxylate; ethyl 4,5 bis(4 methoxyphenyl) 1 (4 nitrophenyl) 1h pyrazole 3 carboxylate; ethyl 4,5 bis(4 methoxyphenyl) 1 (4 sulfamoylphenyl) 1h pyrazole 3 carboxylate; ethyl 4,5 bis(4 methoxyphenyl) 1 [4 (trifluoromethyl)phenyl] 1h pyrazole 3 carboxylate; ethyl 4,5 diphenyl 1 (4 sulfamoylphenyl) 1h pyrazole 3 carboxylate; ethyl 4,5 diphenyl 1 [4 (trifluoromethyl)phenyl] 1h pyrazole 3 carboxylate; ethyl 5 (2,4 dihydroxyphenyl) 4 phenyl 1 (4 sulfamoylphenyl) 1h pyrazole 3 carboxylate; ethyl 5 (2,4 dimethoxyphenyl) 4 phenyl 1 (4 sulfamoylphenyl) 1h pyrazole 3 carboxylate; ethyl 5 (4 bromophenyl) 1 (4 cyanophenyl) 4 phenyl 1h pyrazole 3 carboxylate; ethyl 5 (4 bromophenyl) 1 (4 methoxyphenyl) 4 phenyl 1h pyrazole 3 carboxylate; ethyl 5 (4 bromophenyl) 1 (4 nitrophenyl) 4 phenyl 1h pyrazole 3 carboxylate; ethyl 5 (4 bromophenyl) 4 phenyl 1 (4 sulfamoylphenyl) 1h pyrazole 3 carboxylate; ethyl 5 (4 bromophenyl) 4 phenyl 1 [4 (trifluoromethyl)phenyl] 1h pyrazole 3 carboxylate; ethyl 5 (4 chlorophenyl) 4 phenyl 1 (4 sulfamoylphenyl) 1h pyrazole 3c arboxylate; ethyl 5 (4 fluorophenyl) 4 phenyl 1 (4 sulfamoylphenyl) 1h pyrazole 3 carboxylate; ethyl 5 (4 hydroxyphenyl) 4 phenyl 1 (4 sulfamoylphenyl) 1h pyrazole 3 carboxylate; n(g) methylarginine; nitric oxide; pyrazole derivative; unclassified drug; antineoplastic agent; bibenzyl derivative; combretastatin; cyclooxygenase 2 inhibitor; lipopolysaccharide; nitric oxide; pyrazole derivative; animal cell; antineoplastic activity; antiproliferative activity; Article; Claisen condensation; controlled study; cytotoxicity; drug design; drug synthesis; Hep-G2 cell line; HT-29 cell line; human; human cell; IC50; Koenigs Knorr reaction; MCF-7 cell line; nonhuman; one pot synthesis; pharmacophore; RAW 264.7 cell line; animal; cell survival; chemistry; cytology; drug effect; drug screening; macrophage; metabolism; mouse; synthesis; tumor cell line; Animals; Antineoplastic Agents; Bibenzyls; Cell Line, Tumor; Cell Survival; Cyclooxygenase 2 Inhibitors; Drug Design; Drug Screening Assays, Antitumor; Humans; Lipopolysaccharides; Macrophages; Mice; Nitric Oxide; Pyrazoles; RAW 264.7 Cells
Tóm tắt tiếng anh
In our efforts to discover novel multi-target agents having better antitumor activities than celecoxib, 21 new aryl-substituted pyrazole derivatives possessing cis-diphenylethylene scaffold were mostly synthesized by a one-pot approach to ethyl 1,4,5-triaryl-1H-pyrazole-3-carboxylates via an improved Claisen condensation – Knorr reaction sequence. The cytotoxic effects of these compounds against three human cancer cell lines HT-29, Hep-G2, MCF-7 as well as their inhibition of NO production were studied. Results showed that incorporation of the important pharmacophoric groups of two original molecules celecoxib and combretastatin A-4 in a single molecule plays an important role in determining a better biological activities of the new coxib-hybrided compounds. © 2019 Wiley-VHCA AG, Zurich, Switzerland
