1403901-49-4Relevant academic research and scientific papers
Discovery of a Potent Nonpeptidomimetic, Small-Molecule Antagonist of Cellular Inhibitor of Apoptosis Protein 1 (cIAP1) and X-Linked Inhibitor of Apoptosis Protein (XIAP)
Tamanini, Emiliano,Buck, Ildiko M.,Chessari, Gianni,Chiarparin, Elisabetta,Day, James E. H.,Frederickson, Martyn,Griffiths-Jones, Charlotte M.,Hearn, Keisha,Heightman, Tom D.,Iqbal, Aman,Johnson, Christopher N.,Lewis, Edward J.,Martins, Vanessa,Peakman, Torren,Reader, Michael,Rich, Sharna J.,Ward, George A.,Williams, Pamela A.,Wilsher, Nicola E.
supporting information, p. 4611 - 4625 (2017/06/13)
XIAP and cIAP1 are members of the inhibitor of apoptosis protein (IAP) family and are key regulators of anti-apoptotic and pro-survival signaling pathways. Overexpression of IAPs occurs in various cancers and has been associated with tumor progression and resistance to treatment. Structure-based drug design (SBDD) guided by structural information from X-ray crystallography, computational studies, and NMR solution conformational analysis was successfully applied to a fragment-derived lead resulting in AT-IAP, a potent, orally bioavailable, dual antagonist of XIAP and cIAP1 and a structurally novel chemical probe for IAP biology.
BICYCLIC HETEROCYCLE COMPOUNDS AND THEIR USES IN THERAPY
-
, (2014/05/07)
The invention relates to new bicyclic heterocycle compounds of formula (I): wherein R1 is seected from specific pyrazolyl, imidazolyl, pridinyl and triazolyl groups. The invention also realtes to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
BICYCLIC HETEROCYCLE COMPOUNDS AND THEIR USES IN THERAPY
-
, (2014/05/07)
The invention relates to new bicyclic heterocycle compounds of formula (I): (Formula (I)), pharmaceutical compositions comprising said compounds and to use of said compounds in the treatment of diseases, e.g. cancer.
BICYCLIC HETEROCYCLE COMPOUNDS AND THEIR USES IN THERAPY
-
, (2014/05/07)
The invention relates to new bicyclic heterocycle compounds of formula (I):,to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
