Synthesis and evaluation of in vitro bioactivity for polysubstituted N-arylpyrazole derivatives

Synthesis and evaluation of in vitro bioactivity for polysubstituted N-arylpyrazole derivatives

New polysubstituted N-arylpyrazole derivatives were synthesized from N1-arylsydnone with acetylene and boronic acid, including 2-thiophenyl, 3-thiophenyl, 2-benzo[b]thiophenyl, or dibenzothiophenyl-4-boronic acid, via 1,3-dipolar cycloaddition and Suzuki coupling reaction. Based on the growth inhibi...

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Bibliographic Details
Main Authors: Naoto Uramaru, En-Chiuan Chang, Wan-Ping Yen, Mou-Yung Yeh, Shin-Hun Juang, Fung Fuh Wong
Format: Article
Language:English
Published: Elsevier 2019-12-01
Series:Arabian Journal of Chemistry
Online Access:http://www.sciencedirect.com/science/article/pii/S187853521400344X
Description
Summary:New polysubstituted N-arylpyrazole derivatives were synthesized from N1-arylsydnone with acetylene and boronic acid, including 2-thiophenyl, 3-thiophenyl, 2-benzo[b]thiophenyl, or dibenzothiophenyl-4-boronic acid, via 1,3-dipolar cycloaddition and Suzuki coupling reaction. Based on the growth inhibitory activity results against lung carcinoma (NCI-H226), nasopharyngeal (NPC-TW01), and T-cell leukemia (Jurkat) cancer cells, compounds 5d and 7d with dibenzothiophenyl bioisostere possessed the significant inhibitory activity for NPC-TW01 (32 μM and 16 μM) and NCI-H226 (16 μM and 8.9 μM), respectively. Keywords: Thiophene, Benzothiophene, Pyrazole, Suzuki coupling reaction, Bioactivity study
ISSN:1878-5352

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