328945-92-2Relevant academic research and scientific papers
A scaffold merging approach to Hsp90 C-terminal inhibition: synthesis and evaluation of a chimeric library
Davis, Rachel E.,Zhang, Zheng,Blagg, Brian S. J.
, p. 593 - 598 (2017)
Inhibition of the Hsp90 C-terminus is an attractive therapeutic paradigm for the treatment of cancer, however the developmental space of C-terminal inhibitors is limited. It was hypothesized that the combination of two previously identified scaffolds into a single structure could provide a platform for which to probe the three-dimensional space within the Hsp90 C-terminal binding pocket. The resulting chimeric compounds displayed anti-proliferative activity at low micromolar concentrations and manifested inhibitory activity in an Hsp90-dependent rematuration assay. Initial structure-activity relationships suggest that this new scaffold binds Hsp90 in a conformation different from that of the parent compounds, and consequently, provides a new opportunity to develop more efficacious inhibitors of the Hsp90 C-terminal binding pocket.
MACROCYCLIC INDOLE DERIVATIVES FOR THE TREATMENT OF HEPATITIS C INFECTIONS
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Page/Page column 37, (2009/03/07)
A class of macrocyclic compounds of formula (I), wherein R7, R9, B, F, M, Q, W, Y and Z are defined herein, that are useful as inhibitors of viral proteases, particularly the hepatitis C virus (HCV) NS3 protease, are provided. Also p
TETRACYCLIC INDOLE DERIVATIVES AS ANTIVIRAL AGENTS
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Page/Page column 35, (2008/06/13)
The present invention relates to tetracyclic indole derivatives of formula (I); wherein Ar, D1, D2, D3, D4, W, X, Y and Z are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical composi
Total syntheses of three natural products, vignafuran, 2-(4-hydroxy-2-methoxyphenyl)-6-methoxybenzofuran-3-carboxylic acid methyl ester, and coumestrol from a common starting material
Hiroya, Kou,Suzuki, Naoyuki,Yasuhara, Akito,Egawa, Yuya,Kasano, Atsushi,Sakamoto, Takao
, p. 4339 - 4346 (2007/10/03)
Vignafuran 2, 2-(4-hydroxy-2-methoxyphenyl)-6-methoxybenzofuran-3-carboxylic acid methyl ester 3, and coumestrol 4 were efficiently synthesized from the same starting material, 4-bromoresorcinol 14a, through the common intermediate, diarylacetylene 7. The key steps of these syntheses were the tetrabutylammonium fluoride (TBAF)-catalyzed benzo[b]furan ring formation for 2 and the carbonylative ring closure methodology catalyzed by a Pd complex for 3 and 4. The Royal Society of Chemistry 2000.
