Design and synthesis of some new tri-substituted pyrazole derivatives as anticancer agents

Design and synthesis of some new tri-substituted pyrazole derivatives as anticancer agents A new series of tri-substituted pyrazole derivatives were designed as anti-cancer agents and synthesized, starting with the formylation of semicarbazone via the Vilsmeier–Haack reaction to give 3-(4-bromophenyl)-1H-pyrazole-4-carbaldehyde I which was the precursor of compounds 1–9. The new chemical entities were screened for their anti-cancer activity on various human cancer cell lines, namely: hepatocellular carcinoma HepG2, breast cancer MCF-7, lung carcinoma A549 and prostatic cancer PC3. Most of the synthesized compounds showed remarkable activity on the tested cell lines, while compound 2 had the highest potency against the HepG2 cell line with an IC50 of 9.13 µM compared with doxorubicin (IC50 = 34.24 µM), the reference standard used in this study, and compound 7 was the most active on the rest of the three cell lines; MCF-7, A549 and PC3 (IC50 = 16.52, 6.52 and 9.13 µM, respectively) relative to IC50 = 20.85, 5.93 and 38.02 µM of the standard. Thus, some of the synthesized tri-substituted pyrazole derivatives, specially 2 and 7, have the potential to be developed into potent anticancer agents. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Research on Chemical Intermediates Springer Journals

Design and synthesis of some new tri-substituted pyrazole derivatives as anticancer agents

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Publisher
Springer Journals
Copyright
Copyright © 2016 by Springer Science+Business Media Dordrecht
Subject
Chemistry; Catalysis; Physical Chemistry; Inorganic Chemistry
ISSN
0922-6168
eISSN
1568-5675
D.O.I.
10.1007/s11164-016-2502-2
Publisher site
See Article on Publisher Site

Abstract

A new series of tri-substituted pyrazole derivatives were designed as anti-cancer agents and synthesized, starting with the formylation of semicarbazone via the Vilsmeier–Haack reaction to give 3-(4-bromophenyl)-1H-pyrazole-4-carbaldehyde I which was the precursor of compounds 1–9. The new chemical entities were screened for their anti-cancer activity on various human cancer cell lines, namely: hepatocellular carcinoma HepG2, breast cancer MCF-7, lung carcinoma A549 and prostatic cancer PC3. Most of the synthesized compounds showed remarkable activity on the tested cell lines, while compound 2 had the highest potency against the HepG2 cell line with an IC50 of 9.13 µM compared with doxorubicin (IC50 = 34.24 µM), the reference standard used in this study, and compound 7 was the most active on the rest of the three cell lines; MCF-7, A549 and PC3 (IC50 = 16.52, 6.52 and 9.13 µM, respectively) relative to IC50 = 20.85, 5.93 and 38.02 µM of the standard. Thus, some of the synthesized tri-substituted pyrazole derivatives, specially 2 and 7, have the potential to be developed into potent anticancer agents.

Journal

Research on Chemical IntermediatesSpringer Journals

Published: Mar 9, 2016

References

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