1246532-45-5Relevant academic research and scientific papers
Synthesis and evaluation of 18F-labeled ATP competitive inhibitors of topoisomerase II as probes for imaging topoisomerase II expression
Daumar, Pierre,Zeglis, Brian M.,Ramos, Nicholas,Divilov, Vadim,Sevak, Kuntal Kumar,Pillarsetty, Nagavarakishore,Lewis, Jason S.
, p. 769 - 781 (2014)
Type II topoisomerase (Topo-II) is an ATP-dependent enzyme that is essential in the transcription, replication, and chromosome segregation processes and, as such, represents an attractive target for cancer therapy. Numerous studies indicate that the respo
HETEROCYCLIC HYDROXAMIC ACIDS AS PROTEIN DEACETYLASE INHIBITORS AND DUAL PROTEIN DEACETYLASE-PROTEIN KINASE INHIBITORS AND METHODS OF USE THEREOF
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, (2016/04/26)
The present invention relates to novel hydroxamic acids which are specific histone deacetylase (HDAC) inhibitors and/or TTK/Mpsl kinase inhibitors, including pharmaceutically acceptable salts thereof, which are useful for modulating HDAC and/or TTK/Mpsl k
Lead optimization of purine based orally bioavailable Mps1 (TTK) inhibitors
Kumar, D. Vijay,Hoarau, Christophe,Bursavich, Matthew,Slattum, Paul,Gerrish, David,Yager, Kraig,Saunders, Michael,Shenderovich, Mark,Roth, Bruce L.,McKinnon, Rena,Chan, Ashley,Cimbora, Daniel M.,Bradford, Chad,Reeves, Leslie,Patton, Scott,Papac, Damon I.,Williams, Brandi L.,Carlson, Robert O.
scheme or table, p. 4377 - 4385 (2012/08/07)
Efforts to optimize biological activity, novelty, selectivity and oral bioavailability of Mps1 inhibitors, from a purine based lead MPI-0479605, are described in this Letter. Mps1 biochemical activity and cytotoxicity in HCT-116 cell line were improved. On-target activity confirmation via mechanism based G2/M escape assay was demonstrated. Physico-chemical and ADME properties were optimized to improve oral bioavailability in mouse.
COMPOUNDS AND THERAPEUTIC USES THEREOF
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Page/Page column 110, (2010/11/03)
The invention relates to compounds, pharmaceutical compositions, and uses thereof, including therapeutic uses thereof, such as methods useful for treating cancer.
