ReviewActa pharmaceutica Sinica. B2019
Structural simplification: an efficient strategy in lead optimization.
Review in Acta pharmaceutica Sinica. B, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 33 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
33 citing papers in PubMed.
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- Design, Synthesis, and Biological Evaluation of Novel Triazine-Based Dual Histone Deacetylase/phosphatidylinositol 3-kinase Inhibitors for Breast Cancer Therapy.ChemMedChem · 2026Article
- Antiviral drug discovery and development: challenges and future directions.Signal transduction and targeted therapy · 2026Review
- Article
- Therapeutic target database 2026: facilitating targeted therapies and precision medicine.Nucleic acids research · 2026Article
- Microbial-Derived Anti-Cancer Compounds: Advances in Drug Discovery, Bioengineering, and Therapeutic Applications.Anti-cancer agents in medicinal chemistry · 2026Review
- Unified Enantioselective Synthesis of 5-Phenylmorphans andOrganic letters · 2025Article
- Design, Synthesis, and Bioactivity Assessment of Modified Vemurafenib Analog.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Digital Alchemy: The Rise of Machine and Deep Learning in Small-Molecule Drug Discovery.International journal of molecular sciences · 2025Review
- Unraveling the therapeutic landscape of approved non-peptide macrocycles.Acta pharmaceutica Sinica. B · 2025Review
- Design and Synthesis of Bis-Chalcones as Curcumin Simplified Analogs and Assessment of Their Antiproliferative Activities Against Human Lung Cancer Cells andPharmaceuticals (Basel, Switzerland) · 2025Article
- Biological and computational assessments of thiazole derivative-reinforced bile salt enriched nano carriers: a new gate in targeting SARS-CoV-2 spike protein.RSC advances · 2024Article
- Structure-activity relationship of pharmacophores and toxicophores: the need for clinical strategy.Daru : journal of Faculty of Pharmacy, Tehran University of Medical Sciences · 2024Review
- In Situ Biofilm Affinity-Based Protein Profiling Identifies the Streptococcal Hydrolase GbpB as the Target of a Carolacton-Inspired Chemical Probe.Journal of the American Chemical Society · 2024Article
- ChemoDOTS: a web server to design chemistry-driven focused libraries.Nucleic acids research · 2024Article
- The Trends and Future Prospective of In Silico Models from the Viewpoint of ADME Evaluation in Drug Discovery.Pharmaceutics · 2023Review
- Carbazole and tetrahydro-carboline derivatives as dopamine DActa pharmaceutica Sinica. B · 2023Article
- Rewiring Drug Research and Development through Human Data-Driven Discovery (HDPharmaceutics · 2023Review
- Quantum Mechanical Assessment of Protein-Ligand Hydrogen Bond Strength Patterns: Insights from Semiempirical Tight-Binding and Local Vibrational Mode Theory.International journal of molecular sciences · 2023Article
Corrections and comments
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Authors and funding
3 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The trend toward designing large hydrophobic molecules for lead optimization is often associated with poor drug-likeness and high attrition rates in drug discovery and development. Structural simplification is a powerful strategy for improving the efficiency and success rate of drug design by avoiding "molecular obesity". The structural simplification of large or complex lead compounds by truncating unnecessary groups can not only improve their synthetic accessibility but also improve their pharmacokinetic profiles, reduce side effects and so on. This review will summarize the application of structural simplification in lead optimization. Numerous case studies, particularly those involving successful examples leading to marketed drugs or drug-like candidates, will be introduced and analyzed to illustrate the design strategies and guidelines for structural simplification.
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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.