82477-67-6Relevant academic research and scientific papers
Synthesis and inhibitory effects of triarylpyrazoles on LPS-induced NO and PGE2 productions in RAW 264.7 macrophages
Park, Byung-Jun,El-Gamal, Mohammed I.,Lee, Woo-Suck,Shin, Ji-Sun,Yoo, Kyung Ho,Lee, Kyung-Tae,Oh, Chang-Hyun
, p. 2161 - 2171 (2017)
Abstract: The inhibition of nitric oxide and prostaglandin E2 productions is a very interesting research topic in the field of anti-inflammatory drug development. In the current study, a new series of 1,3,4-triarylpyrazole derivatives was synth
Discovery of highly potent V600E-B-RAF kinase inhibitors: Molecular modeling study
Tarazi, Hamadeh,El-Gamal, Mohammed I.,Oh, Chang-Hyun
, p. 655 - 663 (2019)
A series of 20 triarylpyrazole derivatives containing amide or urea linker have been synthesized. Their in vitro antiproliferative activity against NCI-60 cancer cell lines panel has been reported. Upon investigating the mechanism of action at molecular l
Synthesis, in vitro antiproliferative activity, and kinase inhibitory effects of pyrazole-containing diarylureas and diarylamides
El-Gamal, Mohammed I.,Park, Byung-Jun,Oh, Chang-Hyun
, p. 230 - 239 (2018)
Twenty pyrazole-containing diarylureas and diarylamides were designed and synthesized. They were tested for in vitro antiproliferative activity over a 58-cancer cell line panel at the NCI, USA. The diarylurea derivatives 1b-e and 1g exerted the strongest
Antiproliferative diarylpyrazole derivatives as dual inhibitors of the ERK pathway and COX-2
El-Gamal, Mohammed I.,Choi, Hong Seok,Yoo, Kyung Ho,Baek, Daejin,Oh, Chang-Hyun
, p. 336 - 347 (2013/09/12)
A series of 3,4-diarylpyrazole-1-carboxamide derivatives was designed and synthesized. A selected group of the target compounds was tested for in vitro antiproliferative activities over a panel of 60 cancer cell lines at the National Cancer Institute (NCI, Bethesda, MD, USA) at a single-dose concentration of 10 μm, and the four most active compounds 9a, 9l, 9n, and 10o were further tested in a five-dose testing mode to determine their IC50 values over the 60 cell lines. In addition, a selected group of target compounds were tested for inhibitory effect over cyclooxygenase isozymes. Compounds 9a, 9l, 9n, and 10o were also tested for MEK and ERK kinase inhibitory activity using Western blot assay. Compound 10o was selective toward melanoma cell line subpanel, and its antiproliferative activity may be attributed to selective cyclooxygenase-2 inhibition and ERK pathway inhibition.
Synthesis of 1H-Pyrazole-1-carboxamide derivatives and their antiproliferative activity against melanoma cell line
El-Gamal, Mohammed I.,Sim, Tae Bo,Hong, Jun Hee,Cho, Jung-Hyuck,Yoo, Kyung Ho,Oh, Chang-Hyun
experimental part, p. 197 - 204 (2011/10/07)
Synthesis of a new series of 1H-pyrazole-1-carboxamide derivatives is described. Their antiproliferative activity against A375 human melanoma cell line was tested and the effect of substituents on the diarylpyrazole scaffold was investigated. The pharmacological results indicated that most of the newly synthesized compounds showed moderate activity against A375, compared with sorafenib. Among all of these derivatives, compound IIe which has N-methylpiperazinyl and phenolic moieties showed the most potent antiproliferative activity against A375 human melanoma cell line.
Discovery and optimization of CRTH2 and DP dual antagonists
Liu, Jiwen,Fu, Zice,Wang, Yingcai,Schmitt, Mike,Huang, Alan,Marshall, Derek,Tonn, George,Seitz, Lisa,Sullivan, Tim,Lucy Tang,Collins, Tassie,Medina, Julio
scheme or table, p. 6419 - 6423 (2010/05/02)
A series of phenylacetic acid derivatives was discovered as CRTH2 antagonists. Modification of the series led to compounds that are also antagonists of DP. Since activation of CRTH2 and DP are believed to play key roles in mediating responses of asthma and other immune diseases, this series was optimized to increase the dual antagonistic activities and improve pharmacokinetic properties. These efforts led to selection of AMG 009 as a clinical candidate.
Substituted Diphenylethers, -Amines, -Sulfides and -Methanes for the Treatment of Respiratory Disease
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Page/Page column 25, (2009/01/20)
The invention relates to substituted diphenylethers, -amines, -sulfides, and -methanes as useful pharmaceutical compounds for treating respiratory-disorders, pharmaceutical compositions containing them, and processes for their preparation.
NOVEL COMPOUNDS
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Page/Page column 40, (2008/06/13)
The invention relates to substituted phenylacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
Mandelic acid derivatives and their use as throbin inhibitors
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Page/Page column 21, (2008/06/13)
There is provided a compound of formula I wherein Ra, R1, R2, Y and R3 have meanings given in the description and pharmaceutically acceptable derivatives (including prodrugs) thereof, which compounds and derivatives are useful as, or are useful as prodrugs of, competitive inhibitors of trypsin-like proteases, such as thrombin, and thus, in particular, in the treatment of conditions where inhibition of thrombin is required (e.g. thrombosis) or as anticoagulants.
PHARMACEUTICAL COMBINATION
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Page 55, (2010/02/04)
There is provided a combination product comprising: (1) a compound of claim 1 in WO 02/44145 or a compound of claim 20 in WO 02/44145 (or derivative thereof)or a pharmaceutically-acceptable derivative thereof; and (1) a compound as defined in claim 1 of WO 01/28992 or (2) a compound of Claim 34 of WO 01/28992 or (3) Compound A or B or C or D (or pharmaceutically-acceptable salts thereof) for use in treating arrhythmia or a coagulation controlled complication thereof.
