622847-16-9Relevant academic research and scientific papers
Discovery and structure-activity relationship of 2-phenyl-oxazole-4-carboxamide derivatives as potent apoptosis inducers
Tai, Vincent W.-F.,Sperandio, David,Shelton, Emma J.,Litvak, Joane,Pararajasingham, Keith,Cebon, Ben,Lohman, Julia,Eksterowicz, John,Kantak, Seema,Sabbatini, Peter,Brown, Cindy,Zeitz, Jennifer,Reed, Chris,Maske, Bill,Graupe, Doris,Estevez, Alberto,Oeh, Jason,Wong, Darren,Ni, Yong,Sprengeler, Paul,Yee, Robert,Magill, Catherine,Neri, Anthony,Cai, Sui Xiong,Drewe, John,Qiu, Ling,Herich, John,Tseng, Ben,Kasibhatla, Shailaja,Spencer, Jeffrey R.
, p. 4554 - 4558 (2006)
As a continuation of our efforts to discover novel apoptosis inducers as anticancer agents using a cell-based caspase HTS assay, 2-phenyl-oxazole-4-carboxamide derivatives were identified. The structure-activity relationships of this class of molecules were explored. Compound 1k, with EC50 of 270 nM and GI50 of 229 nM in human colorectal DLD-1 cells, was selected and demonstrated the ability to cleave PARP and displayed DNA laddering, the hallmarks of apoptosis. Compound 1k showed 63% tumor growth inhibition in human colorectal DLD-1 xenograft mouse model at 50 mpk, bid.
ACETYLENE DERIVATIVES AS INHIBITORS OF HISTONE DEACETYLASE
-
Page/Page column 43, (2010/02/11)
The present invention is directed to certain hydroxamate derivatives that are inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.
