Literature DB >> 24721727

Synthesis and biological evaluation of 2,3-diaryl isoquinolinone derivatives as anti-breast cancer agents targeting ERα and VEGFR-2.

Zhichao Tang1, Shaoxiong Niu1, Fei Liu1, Kejing Lao1, Jingshan Miao2, Jinzi Ji2, Xiang Wang2, Ming Yan2, Luyong Zhang2, Qidong You1, Hong Xiao3, Hua Xiang4.   

Abstract

The estrogen receptor α is recognized as important pharmaceutical target for breast cancer therapy, and vascular endothelial growth factor receptors (VEGFRs) play important roles in tumor angiogenesis including breast cancer. A series of 2,3-diaryl isoquinolinone derivatives were designed and synthesized targeting both estrogen receptor α (ERα) and VEGFR-2. Bioactivity evaluation showed that compounds 7c, 7d and 7f exhibited significant anti-proliferative and anti-angiogenesis activities via ERα and VEGFR-2 dependent mechanisms.
Copyright © 2014 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  2,3-Diaryl isoquinolinone derivatives; Anti-breast cancer; ERα; Synthesis; VEGFR-2

Mesh：

Substances：

Year:  2014        PMID： 24721727     DOI： 10.1016/j.bmcl.2014.03.042

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


  6 in total

1.  The transcriptomic response of cells to a drug combination is more than the sum of the responses to the monotherapies.

Authors:  Jennifer El Diaz; Mehmet Eren Ahsen; Thomas Schaffter; Xintong Chen; Ronald B Realubit; Charles Karan; Andrea Califano; Bojan Losic; Gustavo Stolovitzky
Journal:  Elife       Date:  2020-09-18       Impact factor: 8.140

2.  SAR of Novel 3-Arylisoquinolinones: meta-Substitution on the Aryl Ring Dramatically Enhances Antiproliferative Activity through Binding to Microtubules.

Authors:  Mai A Elhemely; Asma A Belgath; Sherihan El-Sayed; Kepa K Burusco; Manikandan Kadirvel; Annalisa Tirella; Katherine Finegan; Richard A Bryce; Ian J Stratford; Sally Freeman
Journal:  J Med Chem       Date:  2022-03-15       Impact factor: 7.446

Review 3.  Estrogen Receptor Ligands: A Review (2013-2015).

Authors:  Shabnam Farzaneh; Afshin Zarghi
Journal:  Sci Pharm       Date:  2016-04-13

4.  A novel 3-acyl isoquinolin-1(2H)-one induces G2 phase arrest, apoptosis and GSDME-dependent pyroptosis in breast cancer.

Authors:  Lei Ma; Mengyao Bian; Hui Gao; Zhi Zhou; Wei Yi
Journal:  PLoS One       Date:  2022-05-12       Impact factor: 3.240

Review 5.  Recent progress on vascular endothelial growth factor receptor inhibitors with dual targeting capabilities for tumor therapy.

Authors:  Yun Liu; Yang Li; Yuxi Wang; Congcong Lin; Dan Zhang; Juncheng Chen; Liang Ouyang; Fengbo Wu; Jifa Zhang; Lei Chen
Journal:  J Hematol Oncol       Date:  2022-07-07       Impact factor: 23.168

Review 6.  Novel Alkaloids from Marine Actinobacteria: Discovery and Characterization.

Authors:  Anne-Sofie De Rop; Jeltien Rombaut; Thomas Willems; Marilyn De Graeve; Lynn Vanhaecke; Paco Hulpiau; Sofie L De Maeseneire; Maarten L De Mol; Wim K Soetaert
Journal:  Mar Drugs       Date:  2021-12-22       Impact factor: 5.118
  6 in total

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