ArticleJournal of enzyme inhibition and medicinal chemistry2019
Synthesis, preliminarily biological evaluation and molecular docking study of new Olaparib analogues as multifunctional PARP-1 and cholinesterase inhibitors.
Article in Journal of enzyme inhibition and medicinal chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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11 citing papers in PubMed.
- Antitumor activity and structure-activity relationship of poly (ADP-ribose) polymerase (PARP)-based dual inhibitors.Journal of enzyme inhibition and medicinal chemistry · 2026Review
- Harnessing Substituted 4-Chlorothieno[2,3-Pharmaceuticals (Basel, Switzerland) · 2026Article
- Unveiling Promising PARP12 Inhibitors through Virtual Screening for Cancer Therapy.Current pharmaceutical design · 2025Article
- Multi-functionalization of reduced graphene oxide nanosheets for tumor theragnosis: Synthesis, characterization, enzyme assay, in-silico study, radiolabeling and in vivo targeting evaluation.Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences · 2024Article
- Iron(III) Complexes with Non-Steroidal Anti-Inflammatory Drugs: Structure, Antioxidant and Anticholinergic Activity, and Interaction with Biomolecules.International journal of molecular sciences · 2023Article
- Seleno-Analogs of Scaffolds Resembling Natural Products a Novel Warhead toward Dual Compounds.Antioxidants (Basel, Switzerland) · 2023Article
- Neuroprotective Effects of PARP Inhibitors inCells · 2022Article
- Studying the Binding Modes of Novel 2-Aminopyridine Derivatives as Effective and Selective c-Met Kinase Type 1 Inhibitors Using Molecular Modeling Approaches.Molecules (Basel, Switzerland) · 2020Article
- Hybrid inhibitors of DNA and HDACs remarkably enhance cytotoxicity in leukaemia cells.Journal of enzyme inhibition and medicinal chemistry · 2020Article
- Identification of probe-quality degraders for Poly(ADP-ribose) polymerase-1 (PARP-1).Journal of enzyme inhibition and medicinal chemistry · 2020Article
- Multitarget Therapeutic Strategies for Alzheimer's Disease: Review on Emerging Target Combinations.BioMed research international · 2020Review
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9 authors.
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Abstract
A series of new Olaparib derivatives was designed and synthesized, and their inhibitory activities against poly (ADP-ribose) polymerases-1 (PARP-1) enzyme and cancer cell line MDA-MB-436 in vitro were evaluated. The results showed that compound 5l exhibited the most potent inhibitory effects on PARP-1 enzyme (16.10 ± 1.25 nM) and MDA-MB-436 cancer cell (11.62 ± 2.15 μM), which was close to that of Olaparib. As a PARP-1 inhibitor had been reported to be viable to neuroprotection, in order to search for new multitarget-directed ligands (MTDLs) for the treatment of Alzheimer's disease (AD), the inhibitory activities of the synthesized compounds against the enzymes AChE (from electric eel) and BChE (from equine serum) were also tested. Compound 5l displayed moderate BChE inhibitory activity (9.16 ± 0.91 μM) which was stronger than neostigmine (12.01 ± 0.45 μM) and exhibited selectivity for BChE over AChE to some degree. Molecular docking studies indicated that 5l could bind simultaneously to the catalytic active of PARP-1, but it could not interact well with huBChE. For pursuit of PARP-1 and BChE dual-targeted inhibitors against AD, small and flexible non-polar groups introduced to the compound seemed to be conducive to improving its inhibitory potency on huBChE, while keeping phthalazine-1-one moiety unchanged which was mainly responsible for PARP-1 inhibitory activity. Our research gave a clue to search for new agents based on AChE and PARP-1 dual-inhibited activities to treat Alzheimer's disease.
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