Concepedia

Lead Compound Optimization

Lead Compound Optimization is a chemical refinement process in drug discovery whereby a biologically active compound identified from natural or synthetic sources is systematically modified to enhance its pharmacological properties, selectivity, and bioavailability while minimizing toxicity for potential therapeutic application in marine pharmacology.

751

Publications

39.8K

Citations

7.4K

Authors

1.1K

Institutions

Publications per year

2017–2026

298

Parents

Publications

751

Crystal structure of SARS-CoV-2 main protease provides a basis for design of improved α-ketoamide inhibitors

Linlin Zhang, Daizong Lin, Xinyuanyuan Sun et al. · Science · 2020 · 3.4K citations · Full text

, , +15

Mitochondria-Targeted Chemotherapeutics: The Rational Design of Gold(I) <i>N</i>-Heterocyclic Carbene Complexes That Are Selectively Toxic to Cancer Cells and Target Protein Selenols in Preference to Thiols

James L. Hickey, Rasha A. Ruhayel, Peter J. Barnard et al. · Journal of the American Chemical Society · 2008 · 583 citations

, , +17

Phenethylthiazolethiourea (PETT) Compounds, a New Class of HIV-1 Reverse Transcriptase Inhibitors. 1. Synthesis and Basic Structure-Activity Relationship Studies of PETT Analogs

Frank W. Bell, Amanda Cantrell, Marita Hoegberg et al. · Journal of Medicinal Chemistry · 1995 · 455 citations · Full text

, , +15

VolSurf: a new tool for the pharmacokinetic optimization of lead compounds

Gabriele Cruciani, Manuel Pastor, Wolfgang Guba · European Journal of Pharmaceutical Sciences · 2000 · 426 citations

, , +11

Sulfoximines as Rising Stars in Modern Drug Discovery? Current Status and Perspective on an Emerging Functional Group in Medicinal Chemistry

Patrick Mäder, Lars Kattner · Journal of Medicinal Chemistry · 2020 · 413 citations · Full text

, , +8

1–5 of 751

Authors

7.4K

  1. EN
    Ettore Novellino

    University of Naples Federico II, Italy

    7 publications · 384 citations

    7

    h-index

  2. ÍA
    Íñigo Angulo‐Barturen

    GlaxoSmithKline (Spain), Spain

    7 publications · 643 citations

    7

    h-index

  3. MB
    Marı́a Belén Jiménez-Dı́az

    GlaxoSmithKline (Spain), Spain

    5 publications · 519 citations

    5

    h-index

  4. FG
    Francisco‐Javier Gamo

    GlaxoSmithKline (Spain), Spain

    5 publications · 576 citations

    5

    h-index

  5. SW
    Sergio Wittlin

    Swiss Tropical and Public Health Institute, Switzerland

    5 publications · 272 citations

    5

    h-index

1–5 of 7.4K

Institutions

1.1K

  1. Chinese Academy of Sciences

    Beijing, China

    16 h-index

    137 publications

    3.3K citations

  2. University of Chinese Academy of Sciences

    Beijing, China

    14 h-index

    58 publications

    2.3K citations

  3. Merck & Co., Inc., Rahway, NJ, USA (United States)

    Rahway, United States

    12 h-index

    213 publications

    5.3K citations

  4. GlaxoSmithKline (United Kingdom)

    London, United Kingdom

    12 h-index

    73 publications

    4.9K citations

  5. Shanghai Institute of Materia Medica

    Pudong, China

    12 h-index

    114 publications

    2.9K citations

  6. China Pharmaceutical University

    Nanjing, China

    12 h-index

    94 publications

    2K citations

  7. Centre National de la Recherche Scientifique

    Paris, France

    11 h-index

    59 publications

    2.6K citations

  8. Chinese Academy of Medical Sciences & Peking Union Medical College

    Beijing, China

    11 h-index

    81 publications

    2K citations

1–8 of 1.1K

Venues

  1. Journal of Medicinal Chemistry

    256 publications · 14.9K citations

    67

    h-index

  2. ACS Medicinal Chemistry Letters

    44 publications · 1.7K citations

    24

    h-index

  3. Bioorganic & Medicinal Chemistry Letters

    37 publications · 1.1K citations

    20

    h-index

  4. European Journal of Medicinal Chemistry

    20 publications · 549 citations

    16

    h-index

  5. ChemMedChem

    19 publications · 1.1K citations

    15

    h-index

1–5