ArticleMolecules (Basel, Switzerland)2023
New 1,2,3-Triazole/1,2,4-triazole Hybrids as Aromatase Inhibitors: Design, Synthesis, and Apoptotic Antiproliferative Activity.
Article in Molecules (Basel, Switzerland), 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.
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Who cites it
10 citing papers in PubMed, 17 citations in OpenAlex.
- Molecular insights into triazole-based compounds for triple-negative breast cancer treatment.Journal of enzyme inhibition and medicinal chemistry · 2026Review
- Triazole-based inhibitors for breast cancer: biological activity, SAR and synthetic strategies.Molecular diversity · 2026Review
- Triazoles as enzyme inhibitors: synthetic advances, mechanism of action, molecular docking studies and structure-activity relationships.Molecular diversity · 2026Review
- Design, synthesis,RSC advances · 2026Article
- Progress in Heterocyclic Hybrids for Breast Cancer Therapy: Emerging Trends, Hybridization Techniques, Mechanistic Pathways and SAR Insights.Mini reviews in medicinal chemistry · 2026Review
- Synthesis and multi-target antiproliferative evaluation of novel 1,2,4-triazole-3-thione analogues against breast cancer:RSC advances · 2025Article
- Mapping the Landscape of Anti-Breast Cancer Drug Discovery in Saudi Arabia: A Bibliometric Analysis (2019-2023).Scientifica · 2025Article
- Design, synthesis, andRSC advances · 2024Article
- Exploration of nonlinear optical properties of 4-methyl-4H-1,2,4-triazol-3-yl)thio)-N-phenylpropanamide based derivatives: experimental and DFT approach.Scientific reports · 2024Article
- Design and synthesis new indole-based aromatase/iNOS inhibitors with apoptotic antiproliferative activity.Frontiers in chemistry · 2024Article
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Authors and funding
6 authors at 5 institutions in 3 countries.
Funding
Abstract
A novel series of 1,2,3-triazole/1,2,4-triazole hybrids 5a, 5b, and 6a-i was designed and synthesized as antiproliferative agents targeting aromatase enzymes. The antiproliferative activity of the new hybrids against four cancer cells was studied using Erlotinib as a control. Compounds 6a and 6b demonstrated the highest antiproliferative activity among these hybrids, with GI50 values of 40 nM and 35 nM, respectively. Compound 6b was the most potent derivative, with a GI50 of 35 nM, comparable to Erlotinib's GI50 of 33 nM. Compound 6b inhibited all cancer cell lines with comparable efficacy to Erlotinib. Compounds 5a, 5b, and 6a-i were tested for inhibitory action against aromatase as a potential target for their antiproliferative activity. Results revealed that compounds 6a and 6b were the most potent aromatase inhibitors, with IC50 values of 0.12 ± 0.01 µM and 0.09 ± 0.01 µM, respectively, being more potent than the reference Ketoconazole (IC50 = 2.6 ± 0.20 µM) but less potent than Letrozole (IC50 = 0.002 ± 0.0002). These findings indicated that compounds 6a and 6b had significant aromatase inhibitory action and are potential antiproliferative candidates. The findings were further linked to molecular docking investigations, which gave models of strong interactions with the aromatase domain for inhibitors with high binding scores.
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