Literature DB >> 22437113

Design and synthesis of naphthoquinone derivatives as antiproliferative agents and 20S proteasome inhibitors.

Kai Xu1, Zhiyan Xiao, Yan Bo Tang, Li Huang, Chin-Ho Chen, Emika Ohkoshi, Kuo-Hsiung Lee.   

Abstract

Fourteen naphthoquinone derivatives (1-14) were designed based on a putative proteasome inhibitor PI-083. These compounds were synthesized and evaluated against A549, DU145, KB, and KBvin tumor cell lines. Six compounds (2, 4, 8, 9, 10, and 13) showed antiproliferative activities comparable to that of PI-083. Among them, compound 8 was confirmed as a 20S proteasome inhibitor in both in vitro and cell-based assays. These findings endorse further optimization efforts based on this structural phenotype to develop potential anticancer drug candidates.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID： 22437113     DOI： 10.1016/j.bmcl.2012.02.086

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


  8 in total

1.  Discovery of novel covalent proteasome inhibitors through a combination of pharmacophore screening, covalent docking, and molecular dynamics simulations.

Authors:  Aibo Li; Haopeng Sun; Lei Du; Xiaoxin Wu; Jianqin Cao; Qidong You; Yuyan Li
Journal:  J Mol Model       Date:  2014-11-14       Impact factor: 1.810

2.  Discovery of Anilino-1,4-naphthoquinones as Potent EGFR Tyrosine Kinase Inhibitors: Synthesis, Biological Evaluation, and Comprehensive Molecular Modeling.

Authors:  Panupong Mahalapbutr; Ronnakorn Leechaisit; Anusit Thongnum; Duangjai Todsaporn; Veda Prachayasittikul; Thanyada Rungrotmongkol; Supaluk Prachayasittikul; Somsak Ruchirawat; Virapong Prachayasittikul; Ratchanok Pingaew
Journal:  ACS Omega       Date:  2022-05-18

3.  Synthesis, Characterization and In-vitro Evaluation of Novel Naphthoquinone Derivatives and Related Imines: Identification of New Anticancer Leads.

Authors:  Sima Golmakaniyoon; Vahid Reza Askari; Khalil Abnous; Afshin Zarghi; Razieh Ghodsi
Journal:  Iran J Pharm Res       Date:  2019       Impact factor: 1.696

Review 4.  Computational Approaches for the Discovery of Human Proteasome Inhibitors: An Overview.

Authors:  Romina A Guedes; Patrícia Serra; Jorge A R Salvador; Rita C Guedes
Journal:  Molecules       Date:  2016-07-16       Impact factor: 4.411

5.  Phenotypic screen for oxygen consumption rate identifies an anti-cancer naphthoquinone that induces mitochondrial oxidative stress.

Authors:  Frances L Byrne; Ellen M Olzomer; Gabriella R Marriott; Lake-Ee Quek; Alice Katen; Jacky Su; Marin E Nelson; Gene Hart-Smith; Mark Larance; Veronica F Sebesfi; Jeff Cuff; Gabriella E Martyn; Elizabeth Childress; Stephanie J Alexopoulos; Ivan K Poon; Maree C Faux; Antony W Burgess; Glen Reid; Joshua A McCarroll; Webster L Santos; Kate Gr Quinlan; Nigel Turner; Daniel J Fazakerley; Naresh Kumar; Kyle L Hoehn
Journal:  Redox Biol       Date:  2019-11-05       Impact factor: 11.799

6.  1H and 13C NMR chemical shifts of 2-n-alkylamino-naphthalene-1,4-diones.

Authors:  Rishikesh Patil; Mahesh Jadhav; Sunita Salunke-Gawali; Dipali N Lande; Shridhar P Gejji; Debamitra Chakravarty
Journal:  Heliyon       Date:  2021-01-28

7.  Chemodivergent synthesis of N-(pyridin-2-yl)amides and 3-bromoimidazo[1,2-a]pyridines from α-bromoketones and 2-aminopyridines.

Authors:  Yanpeng Liu; Lixue Lu; Haipin Zhou; Feijie Xu; Cong Ma; Zhangjian Huang; Jinyi Xu; Shengtao Xu
Journal:  RSC Adv       Date:  2019-10-28       Impact factor: 4.036

8.  Synthesis and characterization of novel unsymmetrical and symmetrical 3-halo- or 3-methoxy-substituted 2-dibenzoylamino-1,4-naphthoquinone derivatives.

Authors:  Yakini Brandy; Nailah Brandy; Emmanuel Akinboye; Malik Lewis; Claudia Mouamba; Seshat Mack; Ray J Butcher; Alan J Anderson; Oladapo Bakare
Journal:  Molecules       Date:  2013-02-04       Impact factor: 4.411
  8 in total

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