Design, synthesis and biological evaluation of flexible and rigid analogs of 4H-1,2,4-triazoles bearing 3,4,5-trimethoxyphenyl moiety as new antiproliferative agents.

Clicks: 809
ID: 57920
2019
Article Quality & Performance Metrics
Overall Quality Improving Quality
85.2 /100
Combines engagement data with AI-assessed academic quality
AI Quality Assessment 🥈 High Quality
84.4 /100
Academic Rigor 92.0%
Novelty 78.0%
Clarity 87.0%
Key Strengths
  • Strong in vitro cytotoxic assay results
  • Identification of potent compounds with selectivity towards cancer cells
  • Mechanism of action investigation through tubulin polymerization inhibition
Areas for Improvement
  • Lack of in vivo studies to confirm the antiproliferative activity
  • Limited investigation of potential side effects or toxicity
  • The scope is limited to trimethoxyphenyl derivatives; broader structural diversity could be explored
AI Recommendations

Future studies should focus on in vivo evaluation of the identified compounds. Further investigation of the selectivity mechanism and potential toxicity is also recommended. Exploring a wider range of structural analogs could lead to the discovery of even more potent and selective anticancer agents.

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2025 Relevance
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0%
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0
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0%
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0%
Interdisciplinary Value
🔀 Cross-disciplinary
68%
Practical Impact Potential
Real-world Applications
75%
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Abstract
Several flexible and rigid analogs of 4H-1,2,4-triazoles (compounds 8a-g and 9a-g) bearing trimethoxyphenyl pharmacophoric unit, were designed and synthesized as potential anticancer agents. The in vitro cytotoxic assay indicated that both flexible and rigid analogs (8 and 9, respectively) can potentially inhibit the growth of cancerous cells (A549, MCF7, and SKOV3), with IC values less than 5.0 µM. Furthermore, compounds 10a-l as regional isomers of compounds 9 exhibited remarkable cytotoxic activity with IC values ranging from 0.30 to 5.0 µM. The rigid analogs 9a, 10h and 10k were significantly more potent than etoposide against MCF7, SKOV3 and A549 cells, respectively. These compounds showed high selectivity towards cancer cells over normal cells, as they had no significant cytotoxicity against L929 cells. In addition, the representative compounds 9a and 10h could inhibit the tubulin polymerization at micro-molar levels. By determining changes in the colchicine-tubulin fluorescence, it was suggested that compound 10h could bind to the tubulin at the colchicine pocket. The molecular docking study further confirmed the inhibitory activity of promising compounds 9a, 10h and 10k on tubulin polymerization through binding to the colchicine-binding site.
Reference Key
ansari2019designbioorganic Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Ansari, Mahsa;Shokrzadeh, Mohammad;Karima, Saeed;Rajaei, Shima;Hashemi, Seyedeh Mahdieh;Mirzaei, Hassan;Fallah, Marjan;Emami, Saeed;
Journal Bioorganic chemistry
Year 2019
DOI
S0045-2068(19)31026-0
URL
Keywords
cytotoxic activity 3,4,5-trimethoxyphenyl 4h-1,2,4-triazoles anticancer agents conformationally constrained

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