Literature DB >> 16890436

Aza-stilbenes as potent and selective c-RAF inhibitors.

Octerloney McDonald1, Karen Lackey, Ronda Davis-Ward, Edgar Wood, Vicente Samano, Patrick Maloney, Felix Deanda, Robert Hunter.   

Abstract

The synthesis of several novel aza-stilbene derivatives was carried out. The compounds were tested for their c-RAF enzyme inhibition. Compound 27 possesses significant potency against c-RAF and demonstrates selectivity over other protein kinases. A hypothesis for the binding mode, activity, and selectivity is proposed.

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Year:  2006        PMID： 16890436     DOI： 10.1016/j.bmcl.2006.07.063

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


  7 in total

1.  THP-1 and Dictyostelium Infection Models for Screening and Characterization of Anti-Mycobacterium abscessus Hit Compounds.

Authors:  Adrian Richter; Tirosh Shapira; Yossef Av-Gay
Journal:  Antimicrob Agents Chemother       Date:  2019-12-20       Impact factor: 5.191

2.  Evaluation of the published kinase inhibitor set to identify multiple inhibitors of bacterial ATP-dependent mur ligases.

Authors:  Martina Hrast; Kaja Rožman; Iza Ogris; Veronika Škedelj; Delphine Patin; Matej Sova; Hélène Barreteau; Stanislav Gobec; Simona Golič Grdadolnik; Anamarija Zega
Journal:  J Enzyme Inhib Med Chem       Date:  2019-12       Impact factor: 5.051

3.  Azologization and repurposing of a hetero-stilbene-based kinase inhibitor: towards the design of photoswitchable sirtuin inhibitors.

Authors:  Christoph W Grathwol; Nathalie Wössner; Sören Swyter; Adam C Smith; Enrico Tapavicza; Robert K Hofstetter; Anja Bodtke; Manfred Jung; Andreas Link
Journal:  Beilstein J Org Chem       Date:  2019-09-16       Impact factor: 2.883

Review 4.  Synthetic approaches toward stilbenes and their related structures.

Authors:  Zulfiqar Ali Khan; Ahsan Iqbal; Sohail Anjum Shahzad
Journal:  Mol Divers       Date:  2017-04-21       Impact factor: 2.943

5.  Synergistic Effect of 1,3,6-Trihydroxy-4,5,7-Trichloroxanthone in Combination with Doxorubicin on B-Cell Lymphoma Cells and Its Mechanism of Action Through Molecular Docking.

Authors:  Isnatin Miladiyah; Emmy Yuanita; Satyo Nuryadi; Jumina Jumina; Sofia Mubarika Haryana; Mustofa Mustofa
Journal:  Curr Ther Res Clin Exp       Date:  2020-01-30

Review 6.  Photoresponsive Small Molecule Inhibitors for the Remote Control of Enzyme Activity.

Authors:  Dóra Laczi; Mark D Johnstone; Cassandra L Fleming
Journal:  Chem Asian J       Date:  2022-04-21

7.  New tools for evaluating protein tyrosine sulfation: tyrosylprotein sulfotransferases (TPSTs) are novel targets for RAF protein kinase inhibitors.

Authors:  Dominic P Byrne; Yong Li; Pawin Ngamlert; Krithika Ramakrishnan; Claire E Eyers; Carrow Wells; David H Drewry; William J Zuercher; Neil G Berry; David G Fernig; Patrick A Eyers
Journal:  Biochem J       Date:  2018-08-14       Impact factor: 3.857
  7 in total

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