On August 27, 2015, Chessari, Gianni; Buck, Ildiko M.; Day, James E. H.; Day, Philip J.; Iqbal, Aman; Johnson, Christopher N.; Lewis, Edward J.; Martins, Vanessa; Miller, Darcey; Reader, Michael; Rees, David C.; Rich, Sharna J.; Tamanini, Emiliano; Vitorino, Marc; Ward, George A.; Williams, Pamela A.; Williams, Glyn; Wilsher, Nicola E.; Woolford, Alison J.-A. published an article.Recommanded Product: 52537-00-5 The title of the article was Fragment-Based Drug Discovery Targeting Inhibitor of Apoptosis Proteins: Discovery of a Non-Alanine Lead Series with Dual Activity Against cIAP1 and XIAP. And the article contained the following:
Inhibitor of apoptosis proteins (IAPs) are important regulators of apoptosis and pro-survival signaling pathways whose deregulation is often associated with tumor genesis and tumor growth. IAPs have been proposed as targets for anticancer therapy, and a number of peptidomimetic IAP antagonists have entered clin. trials. Using the fragment-based screening approach, the authors identified nonpeptidic fragments binding with millimolar affinities to both cellular inhibitor of apoptosis protein 1 (cIAP1) and X-linked inhibitor of apoptosis protein (XIAP). Structure-based hit optimization together with an anal. of protein-ligand electrostatic potential complementarity allowed us to significantly increase binding affinity of the starting hits. Subsequent optimization gave a potent nonalanine IAP antagonist I structurally distinct from all IAP antagonists previously reported. The lead compound had activity in cell-based assays and in a mouse xenograft efficacy model and represents a highly promising start point for further optimization. The experimental process involved the reaction of 6-Chloro-2,3-dihydro-1H-indole(cas: 52537-00-5).Recommanded Product: 52537-00-5
The Article related to inhibitor apoptosis protein antitumor neoplasm, Pharmacology: Structure-Activity and other aspects.Recommanded Product: 52537-00-5
Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles