Design, synthesis and anticervical cancer activity of new benzofuran-pyrazol-hydrazono- thiazolidin-4-one hybrids as potential EGFR inhibitors and apoptosis inducing agents.

Clicks: 768
ID: 4043
2019
Article Quality & Performance Metrics
Overall Quality Improving Quality
82.4 /100
Combines engagement data with AI-assessed academic quality
AI Quality Assessment 🥈 High Quality
82.8 /100
Academic Rigor 88.0%
Novelty 78.0%
Clarity 85.0%
Key Strengths
  • Identification of a promising anti-cervical cancer compound (14)
  • Comprehensive in vitro analysis including cell cycle, apoptosis, and EGFR inhibition assays
  • Molecular docking study to rationalize the inhibitory activity
Areas for Improvement
  • Lack of in vivo validation
  • Limited exploration of other potential targets besides EGFR
  • The study focuses primarily on one compound (14); further investigation of other active compounds could be beneficial
AI Recommendations

Future studies should focus on in vivo validation of compound 14, exploring its efficacy and toxicity in animal models. Investigating the effects of compound 14 on other relevant signaling pathways in cervical cancer cells could provide a more comprehensive understanding of its mechanism of action. Further optimization of the benzofuran-pyrazol-hydrazono-thiazolidin-4-one scaffold could lead to the development of even more potent anti-cancer agents.

Enhanced v2.0 Analysis NISO/DORA Compliant
NISO/DORA Compliant
High Impact
📊 Established
Topic Trend
2025 Relevance
Relevance
0%
Importance
0%
Authorship
Unknown
Authors
0
Diversity
0%
Research Integrity
COPE Standards
Integrity
0%
Innovation
0%
Interdisciplinary Value
🔀 Cross-disciplinary
68%
Practical Impact Potential
Real-world Applications
75%
Enhanced Evaluation v2.0: Following NISO RP-25-2016, DORA 2025, and COPE assessment standards with 13 quality dimensions.
Readership in this journal
Steady

Ranked #3 of 133 articles by views in Bioorganic chemistry

Most read Least read

Bar heights use a square-root scale. Only the 120 most-read articles are drawn; the journal has 133 in total.

Mint this article as an NFT
Not yet minted

Create a permanent, verifiable on-chain record of this article on the Scimatic Network. The NFT is held in your Journament account, and you can withdraw it to your own wallet at any time.

5 SUSD one-off · no wallet required
Sign in to mint
Abstract
This study represents the synthetic approaches of a new set of 2-(((3-(benzofuran-2-yl)-1-phenyl-1H-pyrazol-4-yl)methylene)hydrazono)-5-(aryl)thiazolidin-4-one derivatives 4-22 aiming to obtain new antiproliferative candidates against human cervix carcinoma cells (Hela) of EGFR PK inhibiting potency. The cancer cells represented promising sensitivity towards the compounds 6, 7, 11, 13, 14, 16, 17 more than or equal to that against the reference drug doxorubicin. In addition, the latter compounds were tested as EGFR protein kinase inhibitors. The results revealed that compound 14 showed more significant EGFR PK inhibitory activity than the reference drug erlotinib (IC50; 0.07, 0.08 µM, respectively). Moreover, cell cycle analysis and apoptosis assay were performed for compound 14 proving its ability to cause G1/S phase arrest and apoptosis in Hela cancer cells, in addition to its activation of the caspases-7 and -3. In addition, derivative 14 increased the expression level of p53 and the ratio of Bax/Bcl-2 which confirmed its mode of action. Molecular docking study of 14 was performed to investigate its binding mode of interaction with EGFR PK in the active site with the aim of rationalizing its promising inhibitory activity. Accordingly, compound 14 might be considered as a promising scaffold anticervical cancer chemotherapeutic and deserves further optimization and in-depth biological studies.
Reference Key
abbas2019designbioorganic Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Abbas, Hebat-Allah S;Abd El-Karim, Somaia S;
Journal Bioorganic chemistry
Year 2019
DOI
S0045-2068(19)30440-7
URL
Keywords Keywords not found

Citations

No citations found. To add a citation, contact the admin at info@scimatic.org

Comments

No comments yet. Be the first to comment on this article.