Literature DB >> 24769346

Synthesis, cytotoxic study and docking based multidrug resistance modulator potential analysis of 2-(9-oxoacridin-10(9H)-yl)-N-phenyl acetamides.

Rajesh Kumar1, Maninder Kaur2, Malkeet Singh Bahia2, Om Silakari3.   

Abstract

The present study describes the synthesis of fifteen 2-(9-oxoacridin-10(9H)-yl)-N-phenyl acetamide derivatives (13a-o) through condensation of 2-chloro-N-phenyl acetamides (12a-o) with acridone molecule (10). All the synthesized compounds were screened for their anti-cancer activity against three diverse cell lines including breast (MCF-7), cervical (HeLa) and lung adenocarcinoma (A-549) employing standard MTT assay. Among synthesized molecules, 13k and 13l showed good cytotoxicity activity against considered three cancer cell lines. Additionally, in silico studies of multidrug resistance modulator (MDR) effects of these compounds was performed by docking simulation in the ATP binding site of P-gp. The results of docking simulation displayed important interactions of these molecules in the active site of this protein and predicted their MDR modulator behavior.
Copyright © 2014 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Acridone derivatives; Cytotoxicity; Docking analysis; MTT assay; Multidrug resistance

Mesh:

Substances:

Year:  2014        PMID: 24769346     DOI: 10.1016/j.ejmech.2014.04.030

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  4 in total

Review 1.  Medicinal chemistry of acridine and its analogues.

Authors:  Parteek Prasher; Mousmee Sharma
Journal:  Medchemcomm       Date:  2018-08-14       Impact factor: 3.597

2.  Synthesis and biological evaluation of 12-N-p-chlorobenzyl sophoridinol derivatives as a novel family of anticancer agents.

Authors:  Chongwen Bi; Cheng Ye; Yinghong Li; Wuli Zhao; Rongguang Shao; Danqing Song
Journal:  Acta Pharm Sin B       Date:  2016-04-14       Impact factor: 11.413

3.  Synthesis, molecular modelling and QSAR study of new N-phenylacetamide-2-oxoindole benzensulfonamide conjugates as carbonic anhydrase inhibitors with antiproliferative activity.

Authors:  Mona F Said; Riham F George; Andrea Petreni; Claudiu T Supuran; Nada M Mohamed
Journal:  J Enzyme Inhib Med Chem       Date:  2022-12       Impact factor: 5.051

4.  Design, synthesis, and biological evaluation of novel N 4 -substituted sulfonamides: acetamides derivatives as dihydrofolate reductase (DHFR) inhibitors.

Authors:  Essam M Hussein; Munirah M Al-Rooqi; Shimaa M Abd El-Galil; Saleh A Ahmed
Journal:  BMC Chem       Date:  2019-07-11
  4 in total

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