Literature DB >> 24798019

Acridone alkaloids from Glycosmis chlorosperma as DYRK1A inhibitors.

Mehdi A Beniddir1, Erell Le Borgne, Bogdan I Iorga, Nadège Loaëc, Olivier Lozach, Laurent Meijer, Khalijah Awang, Marc Litaudon.   

Abstract

Two new acridone alkaloids, chlorospermines A and B (1 and 2), were isolated from the stem bark of Glycosmis chlorosperma, together with the known atalaphyllidine (3) and acrifoline (4), by means of bioguided isolation using an in vitro enzyme assay against DYRK1A. Acrifoline (4) and to a lesser extent chlorospermine B (2) and atalaphyllidine (3) showed significant inhibiting activity on DYRK1A with IC50's of 0.075, 5.7, and 2.2 μM, respectively. Their selectivity profile was evaluated against a panel of various kinases, and molecular docking calculations provided structural details for the interaction between these compounds and DYRK1A.

Entities:  

Mesh：

Substances：

Year:  2014        PMID： 24798019     DOI： 10.1021/np400856h

Source DB:  PubMed          Journal:  J Nat Prod        ISSN： 0163-3864            Impact factor:   4.050


  6 in total

1.  Synthesis and Anticancer Properties of New 3-Methylidene-1-sulfonyl-2,3-dihydroquinolin-4(1H)-ones.

Authors:  Agata Jaskulska; Katarzyna Gach-Janczak; Joanna Drogosz-Stachowicz; Tomasz Janecki; Anna Ewa Janecka
Journal:  Molecules       Date:  2022-06-03       Impact factor: 4.927

Review 2.  Current pharmacotherapy and putative disease-modifying therapy for Alzheimer's disease.

Authors:  Akanksha Kulshreshtha; Poonam Piplani
Journal:  Neurol Sci       Date:  2016-06-01       Impact factor: 3.307

3.  Several human cyclin-dependent kinase inhibitors, structurally related to roscovitine, are new anti-malarial agents.

Authors:  Sandrine Houzé; Nha-Thu Hoang; Olivier Lozach; Jacques Le Bras; Laurent Meijer; Hervé Galons; Luc Demange
Journal:  Molecules       Date:  2014-09-23       Impact factor: 4.411

4.  Probing the Inhibition of Microtubule Affinity Regulating Kinase 4 by N-Substituted Acridones.

Authors:  Maria Voura; Parvez Khan; Savvas Thysiadis; Sotiris Katsamakas; Aarfa Queen; Gulam Mustafa Hasan; Sher Ali; Vasiliki Sarli; Md Imtaiyaz Hassan
Journal:  Sci Rep       Date:  2019-02-08       Impact factor: 4.379

5.  A concise and efficient synthesis of benzimidazo[1,2-c]quinazolines through CuI-catalyzed intramolecular N-arylations.

Authors:  Xinlong Pang; Chao Chen; Ming Li; Chanjuan Xi
Journal:  Beilstein J Org Chem       Date:  2015-11-30       Impact factor: 2.883

6.  Synthesis of novel cytotoxic tetracyclic acridone derivatives and study of their molecular docking, ADMET, QSAR, bioactivity and protein binding properties.

Authors:  Rajkumar Veligeti; Rajesh Bagepalli Madhu; Jayashree Anireddy; Visweswara Rao Pasupuleti; Vijaya Kumar Reddy Avula; Krishna S Ethiraj; Srinivas Uppalanchi; Sivaprasad Kasturi; Yogeeswari Perumal; Hasitha Shilpa Anantaraju; Naveen Polkam; Mallilkarjuna Reddy Guda; Swetha Vallela; Grigory Vasilievich Zyryanov
Journal:  Sci Rep       Date:  2020-11-26       Impact factor: 4.379
  6 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.