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Updated: May 5, 2026
Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis, characterization and anticancer screening of some novel piperonyl-tetrazole derivatives
Mohammad Arshad1, Abdul Roouf Bhat2, Smritee Pokharel2
1Centre for Interdisciplinary Research in Basic Sciences, Jamia Millia Islamia, New Delhi 110025, India.
Abstract:
A series of new 1,2-substituted tetrazole derivatives were synthesized and evaluated on MCF-7 (ER positive), MDA-MB-231 and ZR-75 (ER negative) breast cancer cell lines. Out of the fourteen compounds, three compounds 10, 12 and 14 showed higher inhibitory effects on MCF-7 cells. Whereas, compound 8 exhibited higher inhibition in MDA-MB-231 and ZR-75 cells at 10(-5) M concentration. Total RNA was extracted and effect of compounds on different marker genes was studied. The gene expression of CD44, BRAC and BAX were significantly affected. The compounds were screened against the HepG2 cell line, to know if they are selectively targeting specific cancers and only 1-10 percent inhibition was found at 10(-5) M concentration.
Insights
New tetrazole derivatives show promise in targeting specific breast cancer cell lines. Compounds 10, 12, 14 inhibited estrogen receptor positive MCF-7 cells, while compound 8 targeted estrogen receptor negative cells.
Area of Science:
- Medicinal Chemistry
- Cancer Biology
- Pharmacology
Background:
- Breast cancer remains a leading cause of mortality worldwide.
- Targeted therapies are crucial for improving patient outcomes.
- Tetrazole derivatives are a class of compounds with potential biological activities.
Purpose of the Study:
- To synthesize and evaluate novel 1,2-substituted tetrazole derivatives for their anticancer activity.
- To determine the selective efficacy of these compounds against different breast cancer subtypes (ER-positive and ER-negative).
- To investigate the impact of these compounds on key cancer-related gene expression.
Main Methods:
- Synthesis of fourteen 1,2-substituted tetrazole derivatives.
- In vitro evaluation of compounds against MCF-7, MDA-MB-231, and ZR-75 breast cancer cell lines.
- Analysis of gene expression changes (CD44, BRAC, BAX) using total RNA extraction.
- Screening against HepG2 cell line to assess cancer selectivity.
Main Results:
- Compounds 10, 12, and 14 demonstrated significant inhibitory effects on MCF-7 (ER-positive) cells.
- Compound 8 showed higher inhibition against MDA-MB-231 and ZR-75 (ER-negative) cells at 10(-5) M.
- Significant alterations in CD44, BRAC, and BAX gene expression were observed.
- Minimal inhibition (<10%) was noted against HepG2 cells, suggesting potential selectivity.
Conclusions:
- The synthesized tetrazole derivatives exhibit differential activity against various breast cancer cell lines.
- Specific compounds show potential as targeted therapeutic agents for distinct breast cancer subtypes.
- Further investigation into the mechanism of action and in vivo efficacy is warranted.
