156349-08-5Relevant academic research and scientific papers
Structure-activity relationships and cancer-cell selective toxicity of novel inhibitors of glioma-associated oncogene homologue 1 (Gli1) mediated transcription
Mahindroo, Neeraj,Connelly, Michele C.,Punchihewa, Chandanamali,Kimura, Hiromichi,Smeltzer, Matthew P.,Wu, Song,Fujii, Naoaki
experimental part, p. 4277 - 4287 (2010/03/01)
We report novel inhibitors of Gli1-mediated transcription as potential anticancer agents. Focused chemical libraries were designed and assessed for inhibition of functional cell-based Gli1-mediated transcription and selective toxicity toward cancer cells. The SAR was revealed, and the selectivity of the lead compounds' inhibition of Gli1-mediated transcription over that of Gli2 was determined. Compound 63 (NMDA298-1), which inhibited Gli1-mediated transcription in C3H10T1/2 cells with an IC50 of 6.9 μM, showed 3-fold selectivity for inhibiting transcription mediated by Gli1 over that by Gli2. Cell-viability assays were performed to evaluate the chemical library in a normal cell line and a panel of cancer cell lines with or without up-regulated expression of the Gli1 gene. These compounds decreased the viability of several cancer cell lines but were less active in the noncancerous BJ-hTERT cells. 2009 American Chemical Society.
Dihydropyrancarboxamides related to zanamivir: A new series of inhibitors of influenza virus sialidases. 1. Discovery, synthesis, biological activity, and structure-activity relationships of 4-guanidino- and 4-amino-4h-pyran-6-carboxamides
Smith, Paul W.,Sollis, Steven L.,Howes, Peter D.,Cherry, Peter C.,Starkey, Lan D.,Cobley, Kevin N.,Weston, Helen,Scicinski, Jan,Merritt, Andrew,Whittington, Andrew,Wyatt, Paul,Taylor, Neil,Green, Darren,Bethell, Richard,Madar, Safia,Fenton, Robert J.,Morley, Peter J.,Pateman, Tony,Beresford, Alan
, p. 787 - 797 (2007/10/03)
4-Amino- and 4-guanidino-4ff-pyran-6-carboxamides 4 and 5 related to zanamivir (GG167) are a new class of inhibitors of influenza virus sialidases. Structure-activity studies reveal that, in general, secondary amides are weak inhibitors of both influenza
