85740-98-3Relevant academic research and scientific papers
Evaluation of the inhibitory effects of pyridylpyrazole derivatives on lps-induced pge2 productions and nitric oxide in murine raw 264.7 macrophages
El-Din, Mahmoud M. Gamal,El-Gamal, Mohammed I.,Kwon, Young-Do,Kim, Su-Yeon,Han, Hee-Soo,Park, Sang-Eun,Oh, Chang-Hyun,Lee, Kyung-Tae,Kim, Hee-Kwon
, (2021/11/08)
A series of thirteen triarylpyrazole analogs were investigated as inhibitors of lipopolysaccharide (LPS)-induced prostaglandin E2 (PGE2 ) and nitric oxide (NO) production in RAW 264.7 macrophages. The target compounds 1a–m have first
Design, synthesis, in vitro potent antiproliferative activity, and kinase inhibitory effects of new triarylpyrazole derivatives possessing different heterocycle terminal moieties
Gamal El-Din, Mahmoud M.,El-Gamal, Mohammed I.,Abdel-Maksoud, Mohammed S.,Yoo, Kyung Ho,Oh, Chang-Hyun
, p. 1534 - 1543 (2019/09/04)
A new series of triarylpyrazole derivatives having different heterocycle terminal groups have been designed and synthesised. Compounds 1h–j and 1l exhibited the highest mean percentage inhibition against the 58 cancer cell lines at a concentration of 10 μ
Design, synthesis, and in vitro antiproliferative and kinase inhibitory effects of pyrimidinylpyrazole derivatives terminating with arylsulfonamido or cyclic sulfamide substituents
Gamal El-Din, Mahmoud M.,El-Gamal, Mohammed I.,Abdel-Maksoud, Mohammed S.,Yoo, Kyung Ho,Baek, Daejin,Choi, Jungseung,Lee, Huiseong,Oh, Chang-Hyun
, p. 111 - 122 (2016/12/14)
A novel series of substituted pyrimidine compounds bearing N-phenylpyrazole and terminating with aryl and cyclic sulfonamido moiety were designed, synthesized, and evaluated in vitro as antiproliferative agents against a panel of 53 cell lines of differen
PLATELET ADP RECEPTOR INHIBITORS
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, (2016/08/17)
no abstract published
3-methoxy-4-chlorobenzoic acid and preparation method thereof
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Paragraph 0024; 0025, (2017/04/03)
The invention discloses 3-methoxy-4-chlorobenzoic acid and a preparation method thereof. The preparation method comprises the following steps: by taking 3-hydroxybenzoic acid as a raw material, firstly halogenating with Cl2, and then directly reacting with monochloromethane for carrying out hydrocarbylation on phenolic hydroxyl group, so that the 3-methoxy-4-chlorobenzoic acid is obtained. The preparation method has the advantages of cheap and available raw materials, simple operation steps, good substituent group location capacity, high product purity and high yield, can be applicable to large-scale industrial production and can produce relatively high economic benefit.
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.
New triarylpyrazoles as broad-spectrum anticancer agents: Design, synthesis, and biological evaluation
El-Gamal, Mohammed I.,Park, Yi Seul,Chi, Dae Yoon,Yoo, Kyung Ho,Oh, Chang-Hyun
, p. 315 - 322 (2013/10/01)
A new series of diarylureas and diarylamides possessing 1,3,4-triarylpyrazole scaffold was designed and synthesized. Their in vitro antiproliferative activities against NCI-60 cell line panel were tested. Most of the compounds showed strong and broad-spec
Preparation of (2E,4E)-2-(2-benzyloxyethyl)-5-(3-methoxy-4-chlorophenyl) penta-2,4-dienal as a key intermediate in the synthesis of strobilurin B
Popovsky,Stepanov,Grigorieva
, p. 1616 - 1621 (2013/11/19)
(2E,4E)-2-(2-Benzyloxyethyl)-5-(4-chloro-3-methoxyphenyl)penta-2,4-dienal was obtained by the condensation of 4-benzyloxybutanal N-tert-butylimine with 4-chloro-3-methoxycinnamic aldehyde with ≥98% configurational purity and 40% yield. When 4-benzyloxy-2-triethylsilylbutanal imine was used, a 7: 3 mixture of the target (2E,4E)-dienal with its (2Z,4E)-isomer was obtained in 60% yield; the latter quantitatively isomerized to the thermodynamically preferable target (2E,4E)-dienal.
New diarylureas and diarylamides containing 1,3,4-triarylpyrazole scaffold: Synthesis, antiproliferative evaluation against melanoma cell lines, ERK kinase inhibition, and molecular docking studies
Choi, Won-Kyoung,El-Gamal, Mohammed I.,Choi, Hong Seok,Baek, Daejin,Oh, Chang-Hyun
experimental part, p. 5754 - 5762 (2012/01/03)
Synthesis of a new series of diarylureas and diarylamides possessing 1,3,4-triarylpyrazole scaffold is described. Their in vitro antiproliferative activities against 9 human melanoma cell lines were tested. Compounds 12, 13, 15, and 21-23 showed the highe
Design, synthesis, and antiproliferative activity of 3,4-diarylpyrazole-1- carboxamide derivatives against melanoma cell line
El-Gamal, Mohammed I.,Choi, Hong Seok,Cho, Hae-Guk,Hong, Jun Hee,Yoo, Kyung Ho,Oh, Chang-Hyun
experimental part, p. 745 - 754 (2012/06/30)
Synthesis of a new series of 3,4-diarylpyrazole-1-carboxamide derivatives is described. Their antiproliferative activity against A375P human melanoma cell line was tested and the effect of substituents on the diarylpyrazole scaffold was investigated. The
