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Extended Abstract

Synthesis, Spectral Characterization, and Anti-Tumor Activity of Some Pyrazole Derivatives †

by
Christina Marie Zalaru
1,*,
Maria Marinescu
1,
Florea Dumitrascu
2,
Constantin Draghici
2,
Rodica Tatia
3,
Lucia Moldovan
3,
Alina Constantinescu
1 and
Irina Dumitrescu
1
1
Department of Organic Chemistry, Biochemistry and Catalysis, Faculty of Chemistry, University of Bucharest, 90-92 Panduri Road, Bucharest Romania, RO-050663 Bucharest, Romania
2
Institute of Organic Chemistry “C.D. Nenitescu”, 202B Spl Independentei, RO-060023 Bucharest, Romania
3
Department of Cellular and Molecular Biology, National Institute of Research and Development for Biological Sciences, 296 Splaiul Independenţei, RO-060031 Bucharest, Romania
*
Author to whom correspondence should be addressed.
†
Presented at the 16th International Symposium “Priorities of Chemistry for a Sustainable Development” PRIOCHEM, Bucharest, Romania, 28–30 October 2020.
Proceedings 2020, 57(1), 98; https://doi.org/10.3390/proceedings2020057098
Published: 18 November 2020
(This article belongs to the Proceedings of The 16th International Symposium “Priorities of Chemistry for a Sustainable Development” PRIOCHEM)
Versions Notes

1. Introduction

Cancer is a terrible disease that is spread around the world. Chemotherapy remains a significant way of treating cancerous diseases. Although some impressive progress has been made in cancer therapy, drug resistance and toxicity, the development of new anticancer chemotherapeutic agents is being sought [1,2].

2. Materials and Methods

Commercial reagents have been used in the synthesis of intermediate pyrazolic compounds. All synthesized pyrazolic compounds were characterized by IR, 1H-NMR 13C-NMR, UV-Vis, MS, elemental analysis, and tested in vitro for their anti-tumor activity.

3. Results

In this study three series of pyrazole derivatives were synthesized in two steps with good yields:
In the first step, pyrazoles reacted with a aqueous 30% formaldehyde solution to give the 1-(hydroxymethyl)pyrazole derivatives [3]. In the second step, the 1-hydroxymethyl-pyrazoles reacted with, aromatic amines giving pyrazole Mannich bases [4,5].
The structures of all compounds were confirmed by 1H, 13C-NMR, FTIR, UV-VIS spectra and elemental analysis.
Some compounds were tested in vitro for their cytotoxic activity on normal NCTC cells, and their anti-tumor activity in a culture of human cervix carcinoma Hep-2 cells at different concentrations of the sample for 48 h.
Some new benzimidazole Mannich bases was synthesized and characterized [6].

References

  1. Cherukupalli, S.; Karpoormath, R.; Chandrasekaran, B.; Hampannavar, G.A.; Thapliyal, N.; Palakollu, V.N. An insight on synthetic and medicinal aspects of pyrazolo[1,5-a] pyrimidine scaffold. Eur. J. Med. Chem. 2017, 126, 298–352. [Google Scholar] [CrossRef] [PubMed]
  2. Hong, D.; Meiling, H.; Jianqiang, Q.; Ji, L.; Chi, M.; Yangyang, L.; Guxu, M.; Ting, Z.; Senling, W.; Yujun, S.; et al. Excellent antitumor and antimetastatic activities based on novelcoumarin/pyrazole oxime hybrids. Eur. J. Med. Chem. 2019, 166, 470–479. [Google Scholar]
  3. Zalaru, C.; Putina, G.; Dumitrascu, F.; Draghici, C. New Mannich bases with pharmacological activity. Rev. Chim. 2007, 58, 773–775. [Google Scholar]
  4. Marinescu, M.; Tudorache, D.G.; Marton, G.I.; Zalaru, C.M.; Popa, M.; Chifiriuc, M.C.; Stavarache, E.; Constantinescu, C. Density functional theory molecular modeling, chemical synthesis, and antimicrobial behavior of selected benzimidazole derivatives. J. Mol. Struct. 2017, 1030, 463–471. [Google Scholar] [CrossRef]
  5. Zalaru, C.; Dumitrascu, F.; Draghici, C.; Tarcomnicu, I.; Tatia, R.; Moldovan, L.; Chifiriuc, M.C.; Lazar, V.; Marinescu, M.; Nitulescu, M.G.; et al. Synthesis, spectroscopic characterization, DFT study and antimicrobial activity of novel alkylaminopyrazole derivatives. J. Mol. Struct. 2018, 1156, 12–21. [Google Scholar] [CrossRef]
  6. Marinescu, M.; Cinteza, L.O.; Marton, G.I.; Chifiriuc, M.C.; Popa, M.; Stanculescu, I.; Zalaru, C.-M.; Stavarache, C.-E. Synthesis, density functional theory study and in vitro antimicrobial evaluation of new benzimidazole Mannich bases. BMC Chem. 2020, 14, 45. [Google Scholar] [CrossRef] [PubMed]
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MDPI and ACS Style

Zalaru, C.M.; Marinescu, M.; Dumitrascu, F.; Draghici, C.; Tatia, R.; Moldovan, L.; Constantinescu, A.; Dumitrescu, I. Synthesis, Spectral Characterization, and Anti-Tumor Activity of Some Pyrazole Derivatives. Proceedings 2020, 57, 98. https://doi.org/10.3390/proceedings2020057098

AMA Style

Zalaru CM, Marinescu M, Dumitrascu F, Draghici C, Tatia R, Moldovan L, Constantinescu A, Dumitrescu I. Synthesis, Spectral Characterization, and Anti-Tumor Activity of Some Pyrazole Derivatives. Proceedings. 2020; 57(1):98. https://doi.org/10.3390/proceedings2020057098

Chicago/Turabian Style

Zalaru, Christina Marie, Maria Marinescu, Florea Dumitrascu, Constantin Draghici, Rodica Tatia, Lucia Moldovan, Alina Constantinescu, and Irina Dumitrescu. 2020. "Synthesis, Spectral Characterization, and Anti-Tumor Activity of Some Pyrazole Derivatives" Proceedings 57, no. 1: 98. https://doi.org/10.3390/proceedings2020057098

APA Style

Zalaru, C. M., Marinescu, M., Dumitrascu, F., Draghici, C., Tatia, R., Moldovan, L., Constantinescu, A., & Dumitrescu, I. (2020). Synthesis, Spectral Characterization, and Anti-Tumor Activity of Some Pyrazole Derivatives. Proceedings, 57(1), 98. https://doi.org/10.3390/proceedings2020057098

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