Literature DB >> 20655216

Using an in vitro cytotoxicity assay to aid in compound selection for in vivo safety studies.

Nigel Greene1, Michael D Aleo, Shirley Louise-May, David A Price, Yvonne Will.   

Abstract

Recent publications have demonstrated that using calculated physiochemical properties can help in the design of compounds that have a decreased risk of significant findings in rodent toxicology studies. In this Letter, we extend this concept and incorporate results from a high throughput cytotoxicity assay to help the drug discovery community select compounds for progression into in vivo studies. The results are presented in an easily interpretable odds ratio so that teams can readily compare compounds and progress potential clinical candidates to the necessary rodent in vivo studies. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20655216     DOI： 10.1016/j.bmcl.2010.06.129

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  9 in total

Review 1.  The influence of the 'organizational factor' on compound quality in drug discovery.

Authors:  Paul D Leeson; Stephen A St-Gallay
Journal:  Nat Rev Drug Discov       Date:  2011-09-30       Impact factor: 84.694

Review 2.  Strategies for Early Prediction and Timely Recognition of Drug-Induced Liver Injury: The Case of Cyclin-Dependent Kinase 4/6 Inhibitors.

Authors:  Emanuel Raschi; Fabrizio De Ponti
Journal:  Front Pharmacol       Date:  2019-10-24       Impact factor: 5.810

3.  A probable means to an end: exploring P131 pharmacophoric scaffold to identify potential inhibitors of Cryptosporidium parvum inosine monophosphate dehydrogenase.

Authors:  Kehinde F Omolabi; Emmanuel A Iwuchukwu; Clement Agoni; Fisayo A Olotu; Mahmoud E S Soliman
Journal:  J Mol Model       Date:  2021-01-09       Impact factor: 1.810

4.  A human liver microphysiology platform for investigating physiology, drug safety, and disease models.

Authors:  Lawrence A Vernetti; Nina Senutovitch; Robert Boltz; Richard DeBiasio; Tong Ying Shun; Albert Gough; D Lansing Taylor
Journal:  Exp Biol Med (Maywood)       Date:  2015-07-22

5.  Innovative Strategies to Develop Chemical Categories Using a Combination of Structural and Toxicological Properties.

Authors:  Monika Batke; Martin Gütlein; Falko Partosch; Ursula Gundert-Remy; Christoph Helma; Stefan Kramer; Andreas Maunz; Madeleine Seeland; Annette Bitsch
Journal:  Front Pharmacol       Date:  2016-09-21       Impact factor: 5.810

6.  Evaluation of a new lymphocyte proliferation assay based on cyclic voltammetry; an alternative method.

Authors:  Mohammad Nikbakht; Babak Pakbin; Gholamreza Nikbakht Brujeni
Journal:  Sci Rep       Date:  2019-03-14       Impact factor: 4.379

7.  Hepatotoxic potential of asarones: in vitro evaluation of hepatotoxicity and quantitative determination in herbal products.

Authors:  Dhavalkumar N Patel; Han K Ho; Liesbet L Tan; Mui-Mui B Tan; Qian Zhang; Min-Yong Low; Cheng-Leng Chan; Hwee-Ling Koh
Journal:  Front Pharmacol       Date:  2015-02-20       Impact factor: 5.810

8.  Prioritization of anti-malarial hits from nature: chemo-informatic profiling of natural products with in vitro antiplasmodial activities and currently registered anti-malarial drugs.

Authors:  Samuel Ayodele Egieyeh; James Syce; Sarel F Malan; Alan Christoffels
Journal:  Malar J       Date:  2016-01-29       Impact factor: 2.979

Review 9.  Key Challenges and Opportunities Associated with the Use of In Vitro Models to Detect Human DILI: Integrated Risk Assessment and Mitigation Plans.

Authors:  Franck A Atienzar; Eric A Blomme; Minjun Chen; Philip Hewitt; J Gerry Kenna; Gilles Labbe; Frederic Moulin; Francois Pognan; Adrian B Roth; Laura Suter-Dick; Okechukwu Ukairo; Richard J Weaver; Yvonne Will; Donna M Dambach
Journal:  Biomed Res Int       Date:  2016-09-05       Impact factor: 3.411
  9 in total

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