Literature DB >> 16990001

Synthesis and biological evaluation of 5-arylamino-6-chloro-1H-indazole-4,7-diones as inhibitors of protein kinase B/Akt.

Jong Hee Ko1, Seung Woo Yeon, Jung Su Ryu, Tae-Yong Kim, Eun-Ha Song, Hea-Jung You, Rae-Eun Park, Chung-Kyu Ryu.   

Abstract

A series of 5-arylamino-6-chloro-1H-indazole-4,7-diones were synthesized and evaluated for their inhibitory activity on protein kinase B/Akt. The compounds exhibited a potent Akt1 inhibitory activity. Further mechanistic study revealed that they might have dual inhibitory effects on both activity and phosphorylation of Akt1 in PC-3 tumor cell line.

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Year:  2006        PMID： 16990001     DOI： 10.1016/j.bmcl.2006.08.120

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


  6 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.  Highly Active Small Aminated Quinolinequinones against Drug-Resistant Staphylococcus aureus and Candida albicans.

Authors:  Hatice Yıldırım; Nilüfer Bayrak; Mahmut Yıldız; Fatıma Nur Yılmaz; Emel Mataracı-Kara; Deepak Shilkar; Venkatesan Jayaprakash; Amaç Fatih TuYuN
Journal:  Molecules       Date:  2022-05-03       Impact factor: 4.927

3.  Discovery of 4-amino-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamides as selective, orally active inhibitors of protein kinase B (Akt).

Authors:  Tatiana McHardy; John J Caldwell; Kwai-Ming Cheung; Lisa J Hunter; Kevin Taylor; Martin Rowlands; Ruth Ruddle; Alan Henley; Alexis de Haven Brandon; Melanie Valenti; Thomas G Davies; Lynsey Fazal; Lisa Seavers; Florence I Raynaud; Suzanne A Eccles; G Wynne Aherne; Michelle D Garrett; Ian Collins
Journal:  J Med Chem       Date:  2010-03-11       Impact factor: 7.446

4.  Cellular Mechanism of Newly Synthesized Indoledione Derivative-induced Immunological Death of Tumor Cell.

Authors:  Su-Jin Oh; Chung-Kyu Ryu; So-Young Baek; Hyunah Lee
Journal:  Immune Netw       Date:  2011-12-31       Impact factor: 6.303

Review 5.  Akt inhibitors in cancer treatment: The long journey from drug discovery to clinical use (Review).

Authors:  George Mihai Nitulescu; Denisa Margina; Petras Juzenas; Qian Peng; Octavian Tudorel Olaru; Emmanouil Saloustros; Concettina Fenga; Demetrios Α Spandidos; Massimo Libra; Aristidis M Tsatsakis
Journal:  Int J Oncol       Date:  2015-12-24       Impact factor: 5.650

6.  Pharmacophore modeling, virtual screening, and molecular docking studies for discovery of novel Akt2 inhibitors.

Authors:  Jia Fei; Lu Zhou; Tao Liu; Xiang-Yang Tang
Journal:  Int J Med Sci       Date:  2013-01-23       Impact factor: 3.738
  6 in total

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