Literature DB >> 17531483

Indolinone based phosphoinositide-dependent kinase-1 (PDK1) inhibitors. Part 1: design, synthesis and biological activity.

Imadul Islam1, Judi Bryant, Yuo-Ling Chou, Monica J Kochanny, Wheeseong Lee, Gary B Phillips, Hongyi Yu, Marc Adler, Marc Whitlow, Elena Ho, Dao Lentz, Mark A Polokoff, Babu Subramanyam, James M Wu, Daguang Zhu, Richard I Feldman, Damian O Arnaiz.   

Abstract

HTS screening identified 1 with micromolar inhibitory activity against PDK1. Optimization of 1 afforded 4i (BX-517) which has single-digit nanomolar activity against PDK1 and excellent selectivity against PKA.

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Year:  2007        PMID： 17531483     DOI： 10.1016/j.bmcl.2007.04.071

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


  8 in total

1.  Synthesis of Novel 3,5-Disubstituted-2-oxindole Derivatives As Antitumor Agents against Human Nonsmall Cell Lung Cancer.

Authors:  Giulia Nesi; Simona Sestito; Valentina Mey; Simona Ricciardi; Marco Falasca; Romano Danesi; Annalina Lapucci; Maria C Breschi; Stefano Fogli; Simona Rapposelli
Journal:  ACS Med Chem Lett       Date:  2013-10-18       Impact factor: 4.345

2.  Genetic and pharmacological inhibition of PDK1 in cancer cells: characterization of a selective allosteric kinase inhibitor.

Authors:  Kumiko Nagashima; Stuart D Shumway; Sriram Sathyanarayanan; Albert H Chen; Brian Dolinski; Youyuan Xu; Heike Keilhack; Thi Nguyen; Maciej Wiznerowicz; Lixia Li; Bart A Lutterbach; An Chi; Cloud Paweletz; Timothy Allison; Youwei Yan; Sanjeev K Munshi; Anke Klippel; Manfred Kraus; Ekaterina V Bobkova; Sujal Deshmukh; Zangwei Xu; Uwe Mueller; Alexander A Szewczak; Bo-Sheng Pan; Victoria Richon; Roy Pollock; Peter Blume-Jensen; Alan Northrup; Jannik N Andersen
Journal:  J Biol Chem       Date:  2010-11-30       Impact factor: 5.157

3.  Structure-based CoMFA and CoMSIA study of indolinone inhibitors of PDK1.

Authors:  Kirandeep Kaur; Tanaji T Talele
Journal:  J Comput Aided Mol Des       Date:  2008-09-09       Impact factor: 3.686

Review 4.  PDK1 inhibitors.

Authors:  Elisa Barile; Surya K De; Maurizio Pellecchia
Journal:  Pharm Pat Anal       Date:  2012-05

5.  Leishmania parasitophorous vacuole membranes display phosphoinositides that create conditions for continuous Akt activation and a target for miltefosine in Leishmania infections.

Authors:  Naixin Zhang; Samiksha Prasad; Charles-Eugene Huyghues Despointes; Jeffrey Young; Peter E Kima
Journal:  Cell Microbiol       Date:  2018-07-31       Impact factor: 3.715

6.  AutoGPA: An Automated 3D-QSAR Method Based on Pharmacophore Alignment and Grid Potential Analysis.

Authors:  Naoyuki Asakawa; Seiichi Kobayashi; Junichi Goto; Noriaki Hirayama
Journal:  Int J Med Chem       Date:  2012-11-26

7.  Design, Synthesis and Biological Activity Evaluation of S-Substituted 1H-5-Mercapto-1,2,4-Triazole Derivatives as Antiproliferative Agents in Colorectal Cancer.

Authors:  Marius Mioc; Sorin Avram; Vasile Bercean; Ludovic Kurunczi; Roxana M Ghiulai; Camelia Oprean; Dorina E Coricovac; Cristina Dehelean; Alexandra Mioc; Mihaela Balan-Porcarasu; Calin Tatu; Codruta Soica
Journal:  Front Chem       Date:  2018-08-23       Impact factor: 5.221

8.  Using a Genetically Encoded Sensor to Identify Inhibitors of Toxoplasma gondii Ca2+ Signaling.

Authors:  Saima M Sidik; Miryam A Hortua Triana; Aditya S Paul; Majida El Bakkouri; Caroline G Hackett; Fanny Tran; Nicholas J Westwood; Raymond Hui; William J Zuercher; Manoj T Duraisingh; Silvia N J Moreno; Sebastian Lourido
Journal:  J Biol Chem       Date:  2016-03-01       Impact factor: 5.157
  8 in total

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