Literature DB >> 15177442

Lead identification of a potent benzopyranone selective estrogen receptor modulator.

Jeffrey A McKie1, Shripad S Bhagwat, Helen Brady, Mary Doubleday, Leah Gayo, Mathew Hickman, Ravi K Jalluri, Sak Khammungkhune, Adam Kois, Deborah Mortensen, Normand Richard, John Sapienza, Graziella Shevlin, Bernd Stein, May Sutherland.   

Abstract

Starting from a phenol screening hit (6), three series of benzopyranone selective estrogen receptor modulators (SERMs) have been designed, synthesized, and analyzed for both estrogen receptor alpha binding affinity and in vitro activity in two cell assays. The lead compound identified, SP500263 (13), was more potent than raloxifene and tamoxifen in a cell-based assay measuring inhibition of interleukin-6 release.

Entities:  

Mesh:

Substances:

Year:  2004        PMID: 15177442     DOI: 10.1016/j.bmcl.2004.04.081

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


  5 in total

1.  In-vitro antiproliferative activity of benzopyranone derivatives in comparison with standard chemotherapeutic drugs.

Authors:  Musiliyu A Musa; John S Cooperwood; M Omar F Khan; Taufiq Rahman
Journal:  Arch Pharm (Weinheim)       Date:  2010-11-29       Impact factor: 3.751

2.  Anti-breast cancer potential of SS5020, a novel benzopyran antiestrogen.

Authors:  Naomi Suzuki; Xiaoping Liu; Y R Santosh Laxmi; Kanako Okamoto; Hyo Jeong Kim; Guangxiang Zhang; John J Chen; Yoshinori Okamoto; Shinya Shibutani
Journal:  Int J Cancer       Date:  2010-10-29       Impact factor: 7.396

Review 3.  A review of coumarin derivatives in pharmacotherapy of breast cancer.

Authors:  Musiliyu A Musa; John S Cooperwood; M Omar F Khan
Journal:  Curr Med Chem       Date:  2008       Impact factor: 4.530

Review 4.  Estrogen receptors alpha (ERα) and beta (ERβ): subtype-selective ligands and clinical potential.

Authors:  Ilaria Paterni; Carlotta Granchi; John A Katzenellenbogen; Filippo Minutolo
Journal:  Steroids       Date:  2014-06-24       Impact factor: 2.668

5.  Antiestrogenic Activity and Possible Mode of Action of Certain New Nonsteroidal Coumarin-4-acetamides.

Authors:  Maha S Almutairi; Areej N Al Suwayyid; Amal Aldarwesh; Omaima M Aboulwafa; Mohamed I Attia
Journal:  Molecules       Date:  2020-03-28       Impact factor: 4.411

  5 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.