ArticleBioorganic chemistry2021
Synthesis of aspirin-curcumin mimic conjugates of potential antitumor and anti-SARS-CoV-2 properties.
Article in Bioorganic chemistry, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 37 citations in OpenAlex.
- Medicinal Chemistry of Small-Molecule c-Met Inhibitors: From Approved Therapies to Emerging Multitarget Anticancer Agents.International journal of molecular sciences · 2026Review
- Design and synthesis of benzothiazole-sulfonate conjugates targeting influenza A (H1N1) and human coronavirus HCoV-229E:RSC advances · 2026Article
- A Novel Series of Flavone-Cinnamic Acid Hybrid Derivatives as Hypoglycemic Agents: Design, Synthesis, and Activity Studies.Chemistry & biodiversity · 2026Article
- Chemical constituents in the rhizome of Curcuma longa and the pharmacological importance of curcumin hybrids.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2026Review
- Aspirin as a neuroprotective scaffold in Alzheimer's disease: inflammation, oxidative stress, and future directions.Molecular biology reports · 2026Review
- Recent advances in piperidones as privileged scaffolds for drug discovery and development.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2026Review
- Antineoplastic 4-piperidone-1-phosphonothioates with potential multi-targeted inhibitory properties.Scientific reports · 2025Article
- Design and synthesis of antiproliferative 2-oxoindolin-3-ylidenes incorporating urea function with potential VEGFR-2 inhibitory properties.Scientific reports · 2025Article
- Aspirin in Cancer Therapy: Pharmacology and Nanotechnology Advances.International journal of nanomedicine · 2025Review
- Indole Compounds in Oncology: Therapeutic Potential and Mechanistic Insights.Pharmaceuticals (Basel, Switzerland) · 2024Review
- Antineoplastic indole-containing compounds with potential VEGFR inhibitory properties.RSC advances · 2024Review
- Design and Synthesis of Aspirin-chalcone Mimic Conjugates as Potential Anticancer Agents.Anti-cancer agents in medicinal chemistry · 2024Article
- A Comprehensive Update of Anti-COVID-19 Activity of Heterocyclic Compounds.Drug design, development and therapy · 2024Review
- Indole-Based Compounds as Potential Drug Candidates for SARS-CoV-2.Molecules (Basel, Switzerland) · 2023Review
- Spirooxindole: A Versatile Biologically Active Heterocyclic Scaffold.Molecules (Basel, Switzerland) · 2023Review
- Modified Curcumins as Potential Drug Candidates for Breast Cancer: An Overview.Molecules (Basel, Switzerland) · 2022Review
- Synthesis and bio-properties of 4-piperidone containing compounds as curcumin mimics.RSC advances · 2022Review
- Synthesis of Potential Antiviral Agents for SARS-CoV-2 Using Molecular Hybridization Approach.Molecules (Basel, Switzerland) · 2022Article
- A new class of half-sandwich ruthenium complexes containing Biginelli hybrids: anticancer and anti-SARS-CoV-2 activities.Chemico-biological interactions · 2022Article
- Development of spiro-3-indolin-2-one containing compounds of antiproliferative and anti-SARS-CoV-2 properties.Scientific reports · 2022Article
Corrections and comments
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Authors and funding
12 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Series of piperidone-salicylate conjugates were synthesized through the reaction of 3E,5E-bis(arylidene)-4-piperidones with the appropriate acid chloride of acetylsalicylate in the presence of triethylamine. All the synthesized conjugates reveal antiproliferative properties against A431 (squamous skin) cancer cell line with potency higher than that of 5-fluorouracil. Many of the synthesized agents also exhibit promising antiproliferative properties against HCT116 (colon) cancer cell line, of which 5o and 5c are the most effective with 12.9, 9.8 folds potency compared with Sunitinib. Promising activity is also shown against MCF7 (breast) cancer cell line with 1.19, 1.12 folds relative to 5-fluorouracil. PI-flow cytometry of compound 5c supports the arrest of cell cycle at G1-phase. However, compound 5o and Sunitinib arrest the cell cycle at S-phase. The synthesized conjugates can be considered as multi-targeted tyrosine kinase inhibitors due to the promising properties against VEGFR-2 and EGFR in MCF7 and HCT116. CDOCKER studies support the EGFR inhibitory properties. Compounds 5p and 5i possessing thienylidene heterocycle are anti-SARS-CoV-2 with high therapeutic indices. Many of the synthesized agents show enhanced COX-1/2 properties than aspirin with better selectivity index towards COX-2 relative to COX-1. The possible applicability of the potent candidates discovered as antitumor and anti-SARS-CoV-2 is supported by the safe profile against normal (non-cancer, RPE1 and VERO-E6) cells.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.