Synthesis and biological evaluation of some novel
N-arylpyrazole derivatives as cytotoxic agents
Received: 25 August 2012 / Accepted: 4 January 2013 / Published online: 26 January 2013
Ó Springer Science+Business Media Dordrecht 2013
Abstract A series of novel N-arylpyrazole derivatives, 5a–5i, were achieved from
substituted phenylacetic acid via Vilsmeier–Haack reaction, hydrolysis, condensa-
tion, and aromatic substitution reaction. Their chemical structures were conﬁrmed
C NMR, FTIR, HRMS, and elemental analysis. The newly syn-
thesized compounds were tested for their in vitro cytotoxic activity against Bel-
7402, KB, HL-60, and BGC-823 cell lines and found to possess moderate activity.
Keywords Synthesis Á N-arylpyrazole Á Cytotoxicity Á Cancer cell lines
Heterocyclic compounds have played very important roles in the development of
medicines and pesticides in recent years and have become the new trend [1, 2].
Pyrazole derivatives in general are well-known nitrogen-containing heterocyclic
compounds, and various procedures have been developed for their synthesis [3–5].
The chemistry of pyrazole derivatives has been the subject of much research due to
their importance in various applications and their widespread potential biological
and pharmacological activities such as antimicrobial [6, 7], anti-cancer [8, 9],
anticonvulsant , antihistaminic , anti-inﬂammatory , antipyretic ,
anti-infective , anti-virus , anti-anxiety , pain relief , etc. [18, 19].
S. Li (&) Á S. Xu Á S. Ding Á J. Zhang (&) Á S. Wang Á X. Li
Chemical Biology Key Laboratory of Hebei Province, Key Laboratory of Medicinal Chemistry
and Molecular Diagnosis, Ministry of Education, College of Chemistry & Environmental Science,
Hebei University, Baoding 071002, People’s Republic of China
Res Chem Intermed (2014) 40:1459–1468