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Published on: June 16, 2019
Cell-specific cytotoxic effect of pyrazole derivatives on breast cancer cell lines MCF7 and MDA-MB-231
T P Lehmann1, J Kujawski2, J Kruk2
1Department of Biochemistry and Molecular Biology, Poznan University of Medical Sciences, Poznan, Poland. tlehmann@ump.edu.pl.
Abstract:
Pyrazoles and their derivatives belong to a class of compounds that demonstrate a great potential in design of anticancer, antiangiogenic, and antimetastatic drugs. Our earlier studies showed that pyrazole derivatives TOSPYRQUIN and TOSIND diminished viability of colorectal adenocarcinoma cells HT-29. Here we demonstrated for the first time in human mammary gland adenocarcinoma cell lines MCF7 and MDA-MB-231 cells the cytotoxic effects of four pyrazole derivatives: TOSIND, PYRIND, METPYRIND, and DIPYR. Three pyrazoles: PYRIND, METPYRIND, and one novel unpublished derivative DIPYR were tested for the first time in living cells. Viability of MCF7 did not significantly change in the presence of TOSIND but it decreased after 72 hours of treatment with PYRIND (IC-50 39.7 ± 5.8 μM). In the presence of METPYRIND the viability was also diminished, while DIPYR increased MCF7 viability after 24 hours of incubation. The viability of MDA-MB-231 cells was strongly decreased by TOSIND (IC-50 17.7 ± 2.7 μM 72 h), and was not influenced by PYRIND and METPYRIND, while DIPYR increased the viability and stimulated the growth of MDA-MB-231 cells. PYRIND, METPYRIND and DIPYR caused a gradual decrease of caspase-3 and caspase-7 activities in MDA-MB-231 cells and there was no influence of TOSIND on the activity of both caspases. Our results open the way to search for other compounds with pendant pyrazole residues in order to increase their cytotoxic activity; especially with regard to its anti-breast cancer activity. It appears that the pyrazoles synthesized by us diminish cell viability in a cell-specific manner. This observation might be useful in designing 'off-DNA' anticancer drugs, compounds which are not harmful to the healthy cells.
Insights
New pyrazole derivatives show potential as anticancer drugs, selectively reducing cancer cell viability. These compounds, including PYRIND, METPYRIND, and DIPYR, offer a promising avenue for developing targeted cancer therapies with minimal harm to healthy cells.
Area of Science:
- Medicinal Chemistry
- Cancer Biology
- Pharmacology
Background:
- Pyrazoles and derivatives are recognized for their potential in developing anticancer, antiangiogenic, and antimetastatic drugs.
- Previous studies indicated that pyrazole derivatives TOSPYRQUIN and TOSIND reduced colorectal adenocarcinoma cell viability.
- This research investigates novel pyrazole derivatives for their effects on breast cancer cell lines.
Purpose of the Study:
- To evaluate the cytotoxic effects of four pyrazole derivatives (TOSIND, PYRIND, METPYRIND, DIPYR) on human mammary gland adenocarcinoma cell lines (MCF7 and MDA-MB-231).
- To assess the impact of these compounds on cell viability and apoptosis-related enzyme activity (caspase-3 and caspase-7).
- To explore the potential of these pyrazoles in developing cell-specific anticancer agents.
Main Methods:
- Human breast cancer cell lines (MCF7 and MDA-MB-231) were treated with four pyrazole derivatives.
- Cell viability was assessed after specific incubation periods (24 and 72 hours).
- Activities of caspase-3 and caspase-7 were measured to evaluate apoptotic effects.
Main Results:
- PYRIND and METPYRIND reduced MCF7 cell viability, while DIPYR increased it.
- TOSIND significantly decreased MDA-MB-231 cell viability (IC-50 17.7 ± 2.7 μM at 72h), whereas PYRIND and METPYRIND had no significant effect.
- DIPYR increased viability and stimulated growth in MDA-MB-231 cells.
- PYRIND, METPYRIND, and DIPYR gradually decreased caspase-3 and caspase-7 activities in MDA-MB-231 cells; TOSIND had no effect.
Conclusions:
- The tested pyrazole derivatives exhibit cell-specific cytotoxic effects against breast cancer cell lines.
- PYRIND, METPYRIND, and DIPYR demonstrate potential for targeted breast cancer therapy.
- These findings support the development of pyrazole-based compounds as 'off-DNA' anticancer drugs with improved safety profiles.
