Literature DB >> 21392984

Discovery and SAR of spirochromane Akt inhibitors.

Nicholas C Kallan1, Keith L Spencer, James F Blake, Rui Xu, Justin Heizer, Josef R Bencsik, Ian S Mitchell, Susan L Gloor, Matthew Martinson, Tyler Risom, Stefan D Gross, Tony H Morales, Wen-I Wu, Guy P A Vigers, Barbara J Brandhuber, Nicholas J Skelton.   

Abstract

A novel series of spirochromane pan-Akt inhibitors is reported. SAR optimization furnished compounds with improved enzyme potencies and excellent selectivity over the related AGC kinase PKA. Attempted replacement of the phenol hinge binder provided compounds with excellent Akt enzyme and cell activities but greatly diminished selectivity over PKA.
Copyright © 2011 Elsevier Ltd. All rights reserved.

Entities:  

Mesh：

Substances：

Year:  2011        PMID： 21392984     DOI： 10.1016/j.bmcl.2011.02.073

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


  8 in total

Review 1.  Inhibition of Akt with small molecules and biologics: historical perspective and current status of the patent landscape.

Authors:  Margrith E Mattmann; Sydney L Stoops; Craig W Lindsley
Journal:  Expert Opin Ther Pat       Date:  2011-06-02       Impact factor: 6.674

2.  Combining ligand- and structure-based in silico methods for the identification of natural product-based inhibitors of Akt1.

Authors:  Priya Mahajan; Bhumika Wadhwa; Manas Ranjan Barik; Fayaz Malik; Amit Nargotra
Journal:  Mol Divers       Date:  2019-02-23       Impact factor: 2.943

3.  Binding selectivity studies of PKBα using molecular dynamics simulation and free energy calculations.

Authors:  Shi-Feng Chen; Yang Cao; Jiong-Jiong Chen; Jian-Zhong Chen
Journal:  J Mol Model       Date:  2013-10-02       Impact factor: 1.810

4.  Efficient and cost effective production of active-form human PKB using silkworm larvae.

Authors:  Ryoko Maesaki; Ryosuke Satoh; Masato Taoka; Teppei Kanaba; Tsunaki Asano; Chiharu Fujita; Toshinobu Fujiwara; Yutaka Ito; Toshiaki Isobe; Toshio Hakoshima; Katsumi Maenaka; Masaki Mishima
Journal:  Sci Rep       Date:  2014-08-15       Impact factor: 4.379

5.  An Improved Free Energy Perturbation FEP+ Sampling Protocol for Flexible Ligand-Binding Domains.

Authors:  Filip Fratev; Suman Sirimulla
Journal:  Sci Rep       Date:  2019-11-14       Impact factor: 4.379

6.  Urolithin A Promotes Angiogenesis and Tissue Regeneration in a Full-Thickness Cutaneous Wound Model.

Authors:  Zhen-Hua Feng; Jia Chen; Pu-Tao Yuan; Zhong-Yin Ji; Si-Yue Tao; Lin Zheng; Xiao-An Wei; Ze-Yu Zheng; Bing-Jie Zheng; Bin Chen; Jian Chen; Feng-Dong Zhao
Journal:  Front Pharmacol       Date:  2022-03-14       Impact factor: 5.810

Review 7.  Drug Discovery of Plausible Lead Natural Compounds That Target the Insulin Signaling Pathway: Bioinformatics Approaches.

Authors:  Siba Shanak; Najlaa Bassalat; Ahmad Barghash; Sleman Kadan; Mahmoud Ardah; Hilal Zaid
Journal:  Evid Based Complement Alternat Med       Date:  2022-03-20       Impact factor: 2.629

8.  Design and Synthesis of Coumarin Derivatives as Cytotoxic Agents through PI3K/AKT Signaling Pathway Inhibition in HL60 and HepG2 Cancer Cells.

Authors:  Safaa M Kishk; Enas E Eltamany; Mohamed S Nafie; Roaa M Khinkar; Rawan H Hareeri; Sameh S Elhady; Asmaa S A Yassen
Journal:  Molecules       Date:  2022-10-09       Impact factor: 4.927
  8 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.