Literature DB >> 17088059

Simplified staurosporine analogs as potent JAK3 inhibitors.

Shyh-Ming Yang1, Ravi Malaviya, Lawrence J Wilson, Rochelle Argentieri, Xin Chen, Cangming Yang, Bingbing Wang, Druie Cavender, William V Murray.   

Abstract

Simplification of bottom ring and regioselective functionalization of the indolocarbazole unit of staurosporine (2) are described. The modification led to a new series of simplified staurosporine analogs, which exhibited significant inhibitory activity against Janus kinase 3 (JAK3). The structure-activity relationships (SAR) are discussed and a proposed binding model is also highlighted.

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Year:  2006        PMID: 17088059     DOI: 10.1016/j.bmcl.2006.10.062

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


  8 in total

1.  JAK2 JH2 Fluorescence Polarization Assay and Crystal Structures for Complexes with Three Small Molecules.

Authors:  Ana S Newton; Luca Deiana; David E Puleo; José A Cisneros; Kara J Cutrona; Joseph Schlessinger; William L Jorgensen
Journal:  ACS Med Chem Lett       Date:  2017-05-17       Impact factor: 4.345

2.  Molecular dynamics and integrated pharmacophore-based identification of dual [Formula: see text] inhibitors.

Authors:  Maninder Kaur; Pankaj Kumar Singh; Manjinder Singh; Renu Bahadur; Om Silakari
Journal:  Mol Divers       Date:  2017-11-14       Impact factor: 2.943

3.  Development of a novel azaspirane that targets the Janus kinase-signal transducer and activator of transcription (STAT) pathway in hepatocellular carcinoma in vitro and in vivo.

Authors:  Chakrabhavi Dhananjaya Mohan; Hanumantharayappa Bharathkumar; Krishna C Bulusu; Vijay Pandey; Shobith Rangappa; Julian E Fuchs; Muthu K Shanmugam; Xiaoyun Dai; Feng Li; Amudha Deivasigamani; Kam M Hui; Alan Prem Kumar; Peter E Lobie; Andreas Bender; Gautam Sethi; Kanchugarakoppal S Rangappa
Journal:  J Biol Chem       Date:  2014-10-15       Impact factor: 5.157

4.  AUDocker LE: A GUI for virtual screening with AUTODOCK Vina.

Authors:  Gaddam Sandeep; Kurre Purna Nagasree; Muppaneni Hanisha; Muthyala Murali Krishna Kumar
Journal:  BMC Res Notes       Date:  2011-10-25

5.  Identification of Potent and Selective JAK1 Lead Compounds Through Ligand-Based Drug Design Approaches.

Authors:  Sathya Babu; Santhosh Kumar Nagarajan; Sruthy Sathish; Vir Singh Negi; Honglae Sohn; Thirumurthy Madhavan
Journal:  Front Pharmacol       Date:  2022-04-21       Impact factor: 5.988

Review 6.  Perspectives for the use of structural information and chemical genetics to develop inhibitors of Janus kinases.

Authors:  Claude Haan; Iris Behrmann; Serge Haan
Journal:  J Cell Mol Med       Date:  2010-01-28       Impact factor: 5.310

7.  Preparation of dibenzo[e,g]isoindol-1-ones via Scholl-type oxidative cyclization reactions.

Authors:  Amy A van Loon; Maeve K Holton; Catherine R Downey; Taryn M White; Carly E Rolph; Stephen R Bruening; Guanqun Li; Katherine M Delaney; Sarah J Pelkey; Erin T Pelkey
Journal:  J Org Chem       Date:  2014-08-25       Impact factor: 4.354

8.  Kinase inhibitors for the treatment of inflammatory and autoimmune disorders.

Authors:  Shripad S Bhagwat
Journal:  Purinergic Signal       Date:  2008-06-21       Impact factor: 3.765

  8 in total

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