18938-22-2Relevant academic research and scientific papers
Synthesis and Biological Evaluation of Novobiocin Core Analogues as Hsp90 Inhibitors
Byrd, Katherine M.,Subramanian, Chitra,Sanchez, Jacqueline,Motiwala, Hashim F.,Liu, Weiya,Cohen, Mark S.,Holzbeierlein, Jeffrey,Blagg, Brian S. J.
, p. 6921 - 6931 (2016)
Development of heat shock protein 90 (Hsp90) C-terminal inhibitors has emerged as an exciting strategy for the treatment of cancer. Previous efforts have focused on modifications to the natural products novobiocin and coumermycin. Moreover, variations in both the sugar and amide moieties have been extensively studied, whereas replacements for the coumarin core have received less attention. Herein, 24 cores were synthesized with varying distances and angles between the sugar and amide moieties. Compounds that exhibited good anti-proliferative activity against multiple cancer cell lines and Hsp90 inhibitory activity, were those that placed the sugar and amide moieties between 7.7 and 12.1 ? apart along with angles of 180°.
SUBSTITUTED UREA DERIVATIVES AND PHARMACEUTICAL USES THEREOF
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Paragraph 0462; 0463; 0464, (2017/12/15)
The present invention is involved in substituted urea derivatives and pharmaceutical uses thereof. Specifically, the present invention provides the mentioned substituted urea derivatives, and its stereoisomer, geometric isomer, tautomer, nitroxide, hydrate, solvate, metabolism product, ester, and pharmaceutically acceptable salt or its prodrug. The present invention also provides the medicament composition comprising the mentioned substituted urea derivatives, and uses of the mentioned substituted urea derivatives or medicament composition in the protection, treatment, curing, or relief of the proliferative diseases of patients, and its use in regulating the activity of protein kinase.
SUBSTITUTED UREA DERIVATIVES AND PHARMACEUTICAL USES THEREOF
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Paragraph 00389, (2016/02/10)
Provided herein are novel substituted urea derivatives, and pharmaceutical compositions thereof. Also provided herein are uses of the compounds or pharmaceutical compositions thereof for preventing, managing, treating or lessening a proliferative disease, andmodulating the activity of protein kinase.
Phenoxide-mediated Sonogashira coupling of trimethylsilylalkynes and aryliodides: Practical synthesis of phenolic-hydroxy-substituted diarylethynes and 1,4-diarylbutadiynes
Shigeta, Masayuki,Watanabe, Junji,Konishi, Gen-Ichi
supporting information, p. 1761 - 1764 (2013/04/10)
We successfully synthesized phenolic-hydroxy-substituted diarylethynes and 1,4-diarylbutadiynes from trimethylsilylalkynes and aryliodides via silyl-group-migration-induced deprotection of alkynes and the usual Sonogashira coupling. The phenol moiety, which works as a desilylating agent, can be attached to any position in the coupling partner. This improvement for Sonogashira coupling would be highly effective, especially when the coupling partner has a phenol moiety. Additionally, the stability of the migrated silyl moiety on the ethynylation of 2-iodophenol is discussed.
Photochromic oxazines with extended conjugation
Petersen, Michael Axman,Deniz, Erhan,Nielsen, Mogens Brondsted,Sortino, Salvatore,Raymo, Francisco M.
supporting information; experimental part, p. 4333 - 4339 (2011/02/24)
We synthesized four compounds with indole and benzooxazine fragments fused in their molecular skeleton and differing in the substituent in the para position, relative to the oxygen atom, of their phenoxy chromophore. This particular substituent extends th
