Scopus Publication Detail
The publication detail shows the title, authors (with indicators showing other profiled authors), information on the publishing organization, abstract and a link to the article in Scopus. This abstract is what is used to create the fingerprint of the publication.
4-Pyridylanilinothiazoles that selectively target von Hippel - Lindau deficient renal cell carcinoma cells by inducing autophagic cell death
Michael P. Hay; Sandra Turcotte; Jack U. Flanagan; Muriel Bonnet; Denise A. Chan; Patrick D. Sutphin; Phuong Nguyen; Amato J. Giaccia; William A. Denny(Profiled Author: Patrick D Sutphin)
Journal of Medicinal Chemistry. 2010;53(2):787-797.Abstract
Renal cell carcinomas (RCC) are refractory to standard therapy with advanced RCC having a poor prognosis; consequently treatment of advanced RCC represents an unmet clinical need. The von Hippel-Lindau (VHL) tumor suppressor gene is mutated or inactivated in a majority of RCCs. We recently identified a 4-pyridyl-2-anilinothiazole (PAT) with selective cytotoxicity against VHL-deficient renal cells mediated by induction of autophagy and increased acidification of autolysosomes. We report exploration of structure-activity relationships (SAR) around this PAT lead. Analogues with substituents on each of the three rings, and various linkers between rings, were synthesized and tested in vitro using paired RCC4 cell lines. A contour map describing the relative spatial contributions of different chemical features to potency illustrates a region, adjacent to the pyridyl ring, with potential for further development. Examples probing this domain validated this approach and may provide the opportunity to develop this novel chemotype as a targeted approach to the treatment of RCC. ©2009 American Chemical Society.
This section shows information related to the publication - computed using the fingerprint of the publication - including related publications, related experts with fingerprints representing significant amounts of overlap between their fingerprint and this publication. The red dots indicate whether those experts or terms appear within the publication, thereby showing potential and actual connections.
Sandra Turcotte; Denise A. Chan; Patrick D. Sutphin; Michael P. Hay; William A. Denny; Amato J. GiacciaCancer Cell. 2008;14(1):90-102.
Sandra Turcotte; Patrick D. Sutphin; Amato J. GiacciaAutophagy. 2008;4(7):944-946.
Patrick D. Sutphin; Denise A. Chan; James M. Li; Sandra Turcotte; Adam J. Krieg; Amato J. GiacciaCancer Research. 2007;67(12):5896-5905.
Appears in this Document