Literature DB >> 20598880

Discovery of novel sphingosine kinase-1 inhibitors. Part 2.

Yibin Xiang1, Bradford Hirth, John L Kane, Junkai Liao, Kevin D Noson, Christopher Yee, Gary Asmussen, Maria Fitzgerald, Christine Klaus, Michael Booker.   

Abstract

Building on our initial work, we have identified additional novel inhibitors of sphingosine kinase-1 (SK1). These new analogs address the shortcomings found in our previously reported compounds. Inhibitors 51 and 54 demonstrated oral bioavailability in a rat PK study. Published by Elsevier Ltd.

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Year:  2010        PMID： 20598880     DOI： 10.1016/j.bmcl.2010.06.019

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


  14 in total

1.  Design, synthesis and biological activity of sphingosine kinase 2 selective inhibitors.

Authors:  Mithun R Raje; Kenneth Knott; Yugesh Kharel; Philippe Bissel; Kevin R Lynch; Webster L Santos
Journal:  Bioorg Med Chem       Date:  2011-11-15       Impact factor: 3.641

2.  Development of amidine-based sphingosine kinase 1 nanomolar inhibitors and reduction of sphingosine 1-phosphate in human leukemia cells.

Authors:  Andrew J Kennedy; Thomas P Mathews; Yugesh Kharel; Saundra D Field; Morgan L Moyer; James E East; Joseph D Houck; Kevin R Lynch; Timothy L Macdonald
Journal:  J Med Chem       Date:  2011-05-02       Impact factor: 7.446

3.  Structure-activity relationship studies and in vivo activity of guanidine-based sphingosine kinase inhibitors: discovery of SphK1- and SphK2-selective inhibitors.

Authors:  Neeraj N Patwardhan; Emily A Morris; Yugesh Kharel; Mithun R Raje; Ming Gao; Jose L Tomsig; Kevin R Lynch; Webster L Santos
Journal:  J Med Chem       Date:  2015-02-13       Impact factor: 7.446

4.  Analysis of selective target engagement by small-molecule sphingosine kinase inhibitors using the Cellular Thermal Shift Assay (CETSA).

Authors:  Jeremy A Hengst; Taryn E Dick; Charles D Smith; Jong K Yun
Journal:  Cancer Biol Ther       Date:  2020-08-23       Impact factor: 4.742

5.  An integrative study to identify novel scaffolds for sphingosine kinase 1 inhibitors.

Authors:  Marcela Vettorazzi; Emilio Angelina; Santiago Lima; Tomas Gonec; Jan Otevrel; Pavlina Marvanova; Tereza Padrtova; Petr Mokry; Pavel Bobal; Lina M Acosta; Alirio Palma; Justo Cobo; Janette Bobalova; Jozef Csollei; Ivan Malik; Sergio Alvarez; Sarah Spiegel; Josef Jampilek; Ricardo D Enriz
Journal:  Eur J Med Chem       Date:  2017-08-10       Impact factor: 6.514

Review 6.  Sphingosine kinase inhibitors: a review of patent literature (2006-2015).

Authors:  Kevin R Lynch; S Brandon Thorpe; Webster L Santos
Journal:  Expert Opin Ther Pat       Date:  2016-08-30       Impact factor: 6.674

Review 7.  Therapeutic potential of targeting sphingosine kinases and sphingosine 1-phosphate in hematological malignancies.

Authors:  C Evangelisti; C Evangelisti; F Buontempo; A Lonetti; E Orsini; F Chiarini; J T Barata; S Pyne; N J Pyne; A M Martelli
Journal:  Leukemia       Date:  2016-07-27       Impact factor: 11.528

8.  An electrophoretic mobility shift assay identifies a mechanistically unique inhibitor of protein sumoylation.

Authors:  Yeong Sang Kim; Katelyn Nagy; Samantha Keyser; John S Schneekloth
Journal:  Chem Biol       Date:  2013-04-18

9.  SKI-178: A Multitargeted Inhibitor of Sphingosine Kinase and Microtubule Dynamics Demonstrating Therapeutic Efficacy in Acute Myeloid Leukemia Models.

Authors:  Jeremy A Hengst; Taryn E Dick; Arati Sharma; Kenichiro Doi; Shailaja Hegde; Su-Fern Tan; Laura M Geffert; Todd E Fox; Arun K Sharma; Dhimant Desai; Shantu Amin; Mark Kester; Thomas P Loughran; Robert F Paulson; David F Claxton; Hong-Gang Wang; Jong K Yun
Journal:  Cancer Transl Med       Date:  2017-08-14

Review 10.  Drugging sphingosine kinases.

Authors:  Webster L Santos; Kevin R Lynch
Journal:  ACS Chem Biol       Date:  2014-11-19       Impact factor: 5.100
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