期刊
MOLECULES
卷 27, 期 18, 页码 -出版社
MDPI
DOI: 10.3390/molecules27185814
关键词
tetra-substituted pyrazoles; mass-spectrometry; antiproliferative activity; computational simulations
资金
- University of Genova
- Italian Ministry of Health
A library of highly functionalized phenylaminopyrazoles was synthesized, characterized, and tested for their cell-based activities, showing potential pharmaceutical applications.
A small library of highly functionalized phenylaminopyrazoles, bearing different substituents at position 1, 3, and 4 of the pyrazole ring, was prepared by the one-pot condensation of active methylene reagents, phenylisothiocyanate, and substituted hydrazine (namely, methyl- and benzyl-hydrazine). The identified reaction conditions proved to be versatile and efficient. Furthermore, the evaluation of alternative stepwise protocols affected the chemo- and regio-selectivity outcome of the one-pot procedure. The chemical identities of two N-methyl pyrazole isomers, selected as prototypes of the whole series, were unambiguously identified by means of NMR and mass spectrometry studies. Additionally, semiempirical calculations provided a structural rationale for the different chromatographic behavior of the two isomers. The prepared tetra-substituted phenylaminopyrazoles were tested in cell-based assays on a panel of cancer and normal cell lines. The tested compounds did not show any cytotoxic effect on the selected cell lines, thus supporting their pharmaceutical potentials.
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