Literature DB >> 20543998

Synthesis and Evaluation of Estradiol Derivatives as Anti-Breast Cancer Agents.

John S Cooperwood1, Jesse Edwards, Musiliyu Musa, Devora Simmons, Abdul D Mian, Kwon-Kyun Park, Zhongliang Wan.   

Abstract

3-N-alkyloxyestradiol derivatives were synthesized, characterized and tested for activity in MCF-7 human breast cancer cells. Among the compounds, the diisopropyl and piperidinyl derivatives were found to be more active than 4-hydroxytamoxifen (HO-Tam), the active metabolite of tamoxifen based upon IC(50) values. The IC(50)s were correlated with structures using molecular modeling.

Entities:  

Year:  2010        PMID： 20543998      PMCID： PMC2882686          DOI： 10.2174/157018010791306551

Source DB:  PubMed          Journal:  Lett Drug Des Discov        ISSN： 1570-1808            Impact factor:   1.150


  14 in total

1.  A general and fast scoring function for protein-ligand interactions: a simplified potential approach.

Authors:  I Muegge; Y C Martin
Journal:  J Med Chem       Date:  1999-03-11       Impact factor: 7.446

2.  Estrogen receptor ligands. Part 1: The discovery of flavanoids with subtype selectivity.

Authors:  Helen Y Chen; Kevin D Dykstra; Elizabeth T Birzin; Katalin Frisch; Wanda Chan; Yi T Yang; Ralph T Mosley; Frank DiNinno; Susan P Rohrer; James M Schaeffer; Milton L Hammond
Journal:  Bioorg Med Chem Lett       Date:  2004-03-22       Impact factor: 2.823

3.  Empirical scoring functions: I. The development of a fast empirical scoring function to estimate the binding affinity of ligands in receptor complexes.

Authors:  M D Eldridge; C W Murray; T R Auton; G V Paolini; R P Mee
Journal:  J Comput Aided Mol Des       Date:  1997-09       Impact factor: 3.686

4.  A fast flexible docking method using an incremental construction algorithm.

Authors:  M Rarey; B Kramer; T Lengauer; G Klebe
Journal:  J Mol Biol       Date:  1996-08-23       Impact factor: 5.469

5.  Development and validation of a genetic algorithm for flexible docking.

Authors:  G Jones; P Willett; R C Glen; A R Leach; R Taylor
Journal:  J Mol Biol       Date:  1997-04-04       Impact factor: 5.469

Review 6.  Endocrine therapy in the treatment of metastatic breast cancer.

Authors:  A U Buzdar
Journal:  Semin Oncol       Date:  2001-06       Impact factor: 4.929

7.  The development of a simple empirical scoring function to estimate the binding constant for a protein-ligand complex of known three-dimensional structure.

Authors:  H J Böhm
Journal:  J Comput Aided Mol Des       Date:  1994-06       Impact factor: 3.686

8.  A geometric approach to macromolecule-ligand interactions.

Authors:  I D Kuntz; J M Blaney; S J Oatley; R Langridge; T E Ferrin
Journal:  J Mol Biol       Date:  1982-10-25       Impact factor: 5.469

9.  Bioactivities, estrogen receptor interactions, and plasminogen activator-inducing activities of tamoxifen and hydroxy-tamoxifen isomers in MCF-7 human breast cancer cells.

Authors:  B S Katzenellenbogen; M J Norman; R L Eckert; S W Peltz; W F Mangel
Journal:  Cancer Res       Date:  1984-01       Impact factor: 12.701

10.  The structural basis of estrogen receptor/coactivator recognition and the antagonism of this interaction by tamoxifen.

Authors:  A K Shiau; D Barstad; P M Loria; L Cheng; P J Kushner; D A Agard; G L Greene
Journal:  Cell       Date:  1998-12-23       Impact factor: 41.582
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  2 in total

1.  Synthesis and biological activity of 3-N-substituted estrogen derivatives as breast cancer agents.

Authors:  Zhongliang Wan; Musiliyu A Musa; Patrick Joseph; John S Cooperwood
Journal:  Mini Rev Med Chem       Date:  2013-07       Impact factor: 3.862

2.  Comparative proteomic analysis reveals growth inhibition by 3-N-alkyloxyestradiol derivative (SERM) in prostate cancer cells.

Authors:  Jennifer E Green; John S Cooperwood; Equar Taka; Karam Fa Soliman; Carl B Goodman; Romonia Renee Reams
Journal:  Cancer Genomics Proteomics       Date:  2014 Jul-Aug       Impact factor: 4.069
  2 in total

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