ACS Medicinal Chemistry Letters, volume 9, issue 2, pages 98-102
Discovery of EBI-2511: A Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkin’s Lymphoma
Lu Biao
1
,
Shen Xiaodong
1
,
Zhang Lei
1
,
Liu Dong
2
,
ZHANG CAIHUA
1
,
Cao Jingsong
2
,
RU SHEN
2
,
Zhang Jiayin
2
,
Wang Dan
1
,
Wan Hong
1
,
Xu Zhibin
1
,
Ho Ming-Hsun
1
,
Zhang Minsheng
2
,
Zhang Lianshan
1
,
Feng He
1
,
Tao Weikang
1
1
Shanghai Hengrui Pharmaceutical Co. Ltd., 279 Wenjing Road, Minhang Hi-tech Zone, Shanghai 200245, China
|
2
Eternity Bioscience Inc., 6 Cedarbrook
Drive, Cranbury, New Jersey 08512, United States
|
Publication type: Journal Article
Publication date: 2018-02-01
Journal:
ACS Medicinal Chemistry Letters
Quartile SCImago
Q1
Quartile WOS
Q2
Impact factor: 4.2
ISSN: 19485875, 19485875
PubMed ID:
29456795
Organic Chemistry
Drug Discovery
Biochemistry
Abstract
A novel series of benzofuran derived EZH2 inhibitors were discovered through a scaffold hopping approach based on the clinical compound of EPZ-6438. Further rational structure-activity relationship exploration and optimization led to the discovery of more potent EZH2 inhibitors with oral bioavailability in mice and rats. A lead compound EBI-2511 (compound 34) demonstrated excellent in vivo efficacy in Pfeiffer tumor Xenograft models in mouse and is under preclinical development for the treatment of cancers associated with EZH2 mutations.
Citations by journals
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1
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3
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Journal of Medicinal Chemistry
3 publications, 10.34%
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European Journal of Medicinal Chemistry
2 publications, 6.9%
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1 publication, 3.45%
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1 publication, 3.45%
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1 publication, 3.45%
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F1000Research
1 publication, 3.45%
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Cancers
1 publication, 3.45%
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1 publication, 3.45%
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Journal of Hematology and Oncology
1 publication, 3.45%
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Biochimica et Biophysica Acta - Gene Regulatory Mechanisms
1 publication, 3.45%
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Tetrahedron Letters
1 publication, 3.45%
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Journal of Organic Chemistry
1 publication, 3.45%
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Bioorganic Chemistry
1 publication, 3.45%
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Medical Oncology
1 publication, 3.45%
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Chemical Record
1 publication, 3.45%
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Helvetica Chimica Acta
1 publication, 3.45%
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RSC Chemical Biology
1 publication, 3.45%
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Expert Opinion on Therapeutic Patents
1 publication, 3.45%
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Molecular Cancer Therapeutics
1 publication, 3.45%
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Topics in Medicinal Chemistry
1 publication, 3.45%
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Medicinal Chemistry Research
1 publication, 3.45%
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New Journal of Chemistry
1 publication, 3.45%
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Experimental and Molecular Medicine
1 publication, 3.45%
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Clinical Epigenetics
1 publication, 3.45%
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Organic Letters
1 publication, 3.45%
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Bioorganic and Medicinal Chemistry Letters
1 publication, 3.45%
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3
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Citations by publishers
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7
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Elsevier
7 publications, 24.14%
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Springer Nature
7 publications, 24.14%
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American Chemical Society (ACS)
5 publications, 17.24%
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Royal Society of Chemistry (RSC)
3 publications, 10.34%
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Wiley
2 publications, 6.9%
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Future Medicine
1 publication, 3.45%
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F1000 Research
1 publication, 3.45%
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Multidisciplinary Digital Publishing Institute (MDPI)
1 publication, 3.45%
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Taylor & Francis
1 publication, 3.45%
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American Association for Cancer Research (AACR)
1 publication, 3.45%
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1
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7
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- We do not take into account publications that without a DOI.
- Statistics recalculated only for publications connected to researchers, organizations and labs registered on the platform.
- Statistics recalculated weekly.
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Lu B. et al. Discovery of EBI-2511: A Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkin’s Lymphoma // ACS Medicinal Chemistry Letters. 2018. Vol. 9. No. 2. pp. 98-102.
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Lu B., Shen X., Zhang L., Liu D., ZHANG C., Cao J., RU S., Zhang J., Wang D., Wan H., Xu Z., Ho M., Zhang M., Zhang L., Feng H., Tao W. Discovery of EBI-2511: A Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkin’s Lymphoma // ACS Medicinal Chemistry Letters. 2018. Vol. 9. No. 2. pp. 98-102.
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TY - JOUR
DO - 10.1021/acsmedchemlett.7b00437
UR - https://doi.org/10.1021/acsmedchemlett.7b00437
TI - Discovery of EBI-2511: A Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkin’s Lymphoma
T2 - ACS Medicinal Chemistry Letters
AU - Shen, Xiaodong
AU - ZHANG, CAIHUA
AU - Cao, Jingsong
AU - RU, SHEN
AU - Zhang, Jiayin
AU - Wan, Hong
AU - Xu, Zhibin
AU - Ho, Ming-Hsun
AU - Zhang, Minsheng
AU - Tao, Weikang
AU - Lu, Biao
AU - Zhang, Lei
AU - Liu, Dong
AU - Wang, Dan
AU - Zhang, Lianshan
AU - Feng, He
PY - 2018
DA - 2018/02/01 00:00:00
PB - American Chemical Society (ACS)
SP - 98-102
IS - 2
VL - 9
PMID - 29456795
SN - 1948-5875
SN - 1948-5875
ER -
Cite this
BibTex
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@article{2018_Lu,
author = {Xiaodong Shen and CAIHUA ZHANG and Jingsong Cao and SHEN RU and Jiayin Zhang and Hong Wan and Zhibin Xu and Ming-Hsun Ho and Minsheng Zhang and Weikang Tao and Biao Lu and Lei Zhang and Dong Liu and Dan Wang and Lianshan Zhang and He Feng},
title = {Discovery of EBI-2511: A Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkin’s Lymphoma},
journal = {ACS Medicinal Chemistry Letters},
year = {2018},
volume = {9},
publisher = {American Chemical Society (ACS)},
month = {feb},
url = {https://doi.org/10.1021/acsmedchemlett.7b00437},
number = {2},
pages = {98--102},
doi = {10.1021/acsmedchemlett.7b00437}
}
Cite this
MLA
Copy
Lu, Biao, et al. “Discovery of EBI-2511: A Highly Potent and Orally Active EZH2 Inhibitor for the Treatment of Non-Hodgkin’s Lymphoma.” ACS Medicinal Chemistry Letters, vol. 9, no. 2, Feb. 2018, pp. 98-102. https://doi.org/10.1021/acsmedchemlett.7b00437.