ArticleRSC advances2023
Novel 4-thiophenyl-pyrazole, pyridine, and pyrimidine derivatives as potential antitumor candidates targeting both EGFR and VEGFR-2; design, synthesis, biological evaluations, and
Article in RSC advances, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 46 citations in OpenAlex.
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- Recent Advances in dehydroacetic acid-clubbed pyridine conjugates: design, synthesis, characterization, molecular docking investigations and evaluation of anti-cancer efficacy.Future medicinal chemistry · 2025Article
- In Silico Identification of Putative Allosteric Pockets and Inhibitors for the KRASG13D-SOS1 Complex in Cancer Therapy.International journal of molecular sciences · 2025Article
- Antiangiogenic potential of phytochemicals from Clerodendrum inerme (L.) Gaertn investigated through in silico and quantum computational methods.Molecular diversity · 2025Article
- Advances in pyrazolo[1,5-RSC advances · 2025Review
- Advances in VEGFR Inhibitors: A Comprehensive Review of Novel Anticancer Agents.Anti-cancer agents in medicinal chemistry · 2025Review
- Synthesis, crystal structure, and antiviral evaluation of new imidazopyridine-schiff base derivatives:RSC advances · 2024Article
- Elaboration of newly synthesized tetrahydrobenzo[b]thiophene derivatives and exploring their antioxidant evaluation, molecular docking, and DFT studies.Scientific reports · 2024Article
- Some pyrimidohexahydroquinoline candidates: synthesis, DFT, cytotoxic activity evaluation, molecular docking, andRSC advances · 2024Article
- Synthesis, toxicological and in silico evaluation of novel spiro pyrimidines against Culex pipiens L. referring to chitinase enzyme.Scientific reports · 2024Article
- Article
- Design, synthesis and evaluation of dihydro-1Journal of enzyme inhibition and medicinal chemistry · 2023Article
- Design and synthesis of new spirooxindole candidates and their selenium nanoparticles as potential dual Topo I/II inhibitors, DNA intercalators, and apoptotic inducers.Journal of enzyme inhibition and medicinal chemistry · 2023Article
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Authors and funding
6 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
In this article, we continued our previous effort to develop new selective anticancer candidates based on the basic pharmacophoric requirements of both EGFR and VEGFR-2 inhibitors. Therefore, twenty-two novel 4-thiophenyl-pyrazole, pyridine, and pyrimidine derivatives were designed and examined as dual EGFR/VEGFR-2 inhibitors. Besides, the previously reported antimicrobial activities of the aforementioned nuclei motivated us to screen their antibacterial and antifungal activities as well. First, the antitumor activities of the newly synthesized derivatives were evaluated against two cancer cell lines (HepG-2 and MCF-7). Notably, compounds 2a, 6a, 7a, 10b, 15a, and 18a exhibited superior anticancer activities against both HepG-2 and MCF-7 cancer cell lines. These candidates were selected to further evaluate their anti-EGFR and anti-VEGFR-2 potentialities which were found to be very promising compared to erlotinib and sorafenib, respectively. Both 10b and 2a derivatives achieved better dual EGFR/VEGFR-2 inhibition with IC
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Registered trials
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