245434-89-3Relevant articles and documents
Isosteres of ester derived glucose uptake inhibitors
Bergmeier, Stephen C.,Chen, Xiaozhuo,Liu, Yi,Qian, Yanrong,Roberts, Dennis A.,Shriwas, Pratik,Wang, Liyi,Zhang, Weihe
, (2020/07/31)
Glucose transporters (GLUTs) facilitate glucose uptake and are overexpressed in most cancer cells. Inhibition of glucose transport has been shown to be an effective method to slow the growth of cancer cells both in vitro and in vivo. We have previously reported on the anticancer activity of an ester derived glucose uptake inhibitor. Due to the hydrolytic instability of the ester linkage we have prepared a series of isosteres of the ester moiety. Of all of the isosteres prepared, the amine linkage showed the most promise. Several additional analogues of the amine-linked compounds were also prepared to improve the overall activity.
Photochemical generation of oxa-dibenzocyclooctyne (ODIBO) for metal-free click ligations
McNitt, Christopher D.,Popik, Vladimir V.
, p. 8200 - 8202,3 (2020/09/09)
Oxa-dibenzocyclooctynes (ODIBO, 2a-c) are prepared by photochemical decarbonylation of corresponding cyclopropenones (photo-ODIBO, 1a-c). While photo-ODIBO does not react with azides, ODIBO is one of the most reactive cyclooctynes exhibiting rates of cycloaddition over 45 M-1 s -1 in aqueous solutions. ODIBO is stable under ambient conditions and has low reactivity towards thiols. Photo-ODIBO survives heating up to 160 °C and does not react with thiols.
Bicyclic aromatic compounds and pharmaceutical/cosmetic compositions comprised thereof
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Page/Page column 32-33, (2010/01/31)
Novel pharmaceutically/cosmetically-active bicyclic aromatic compounds have the structural formula (I): in which Ar1 is a radical having one of the structural formulae (a)-(c): Ar2 is a radical having one of the following formulae (d)-(h): and X is a radical having one of the following formulae (i)-(l): and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.