Amide prodrug derivatives as protein kinase inhibitors
The invention relates to amide prodrug compounds of novel kinase inhibitors. The prodrugs are characterized in that amino of original drugs is subjected to amidation modification, so that bioavailability of the original drugs in vivo is significantly improved. The invention further relates to pharmaceutical composition containing the prodrugs and a method for treating cancer or other cell proliferative abnormal diseases by the prodrugs and the pharmaceutical composition.
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Paragraph 0177; 0184-0187
(2019/02/04)
Enantioselective oxidation by a cyclohexanone monooxygenase from the xenobiotic-degrading Polaromonas sp. strain JS666
A cyclohexanone monooxygenase (CHMO) from the xenobiotic-degrading Polaromonas sp. strain JS666 was heterologously expressed in Escherichia coli, and its ability to catalyze enantio- and regiodivergent oxidations of prochiral and racemic ketones was investigated. The expression system was also used to evaluate this enzyme's potential role in the oxidation of cis-1,2-dichloroethene (cDCE), a groundwater pollutant for which strain JS666 is the only known assimilator. The substrate enantiopreference and -selectivity of the strain JS666 CHMO is similar to that of other CHMO-type enzymes; of note is this enzyme's excellent stereodiscrimination of 2-substituted cyclic ketones. The expression system exhibits no activity with ethene or cDCE as substrates under the tested conditions. Phylogenetic analysis shows that sequence variability among cyclohexanone monooxygenases could be a rich source of new enzyme activities and attributes.
Alexander, Anne K.,Biedermann, David,Fink, Michael J.,Mihovilovic, Marko D.,Mattes, Timothy E.
experimental part
p. 105 - 110
(2012/07/28)
A simple and efficient synthesis of 1,4-And 1,5-dioxepan-2-one
A novel synthesis of 1,4-and 1,5-dioxepan-2-one lactones was achieved through the regioselective oxidation of 3-(2-hydroxyethoxy)propan-1-ol. Under basic conditions, when 3-(2-hydroxyethoxy)propan-1-ol was oxidized using oxoammonium salts, a quantitative
Hassannia, Ali,Piercy, Graeme,Merbouh, Nabyl
experimental part
p. 478 - 480
(2010/04/23)
Stereoselective desymmetrizations by recombinant whole cells expressing the Baeyer-Villiger monooxygenase from Xanthobacter sp. ZL5: A new biocatalyst accepting structurally demanding substrates
In this work the substrate profile and stereoselectivity of engineered whole cells overexpressing the Baeyer-Villiger monooxygenase from Xanthobacter sp. ZL5 with respect to biotransformations of prochiral substrates is characterized. This enzyme catalyzes the desymmetrization of cyclic ketones bearing different chemical features with stereoselectivity similar to that obtained with a related protein from Acinetobacter as a prototype representative of the cyclohexanone monooxygenase enzyme cluster. Moreover, this biocatalyst is able to convert sterically demanding substrates previously not transformed by other enzymes with excellent enantioselectivities. These results expand the repertoire of optically pure lactones accessible by whole-cell biotransformation processes, which are useful intermediates for the synthesis of natural and bioactive products. In addition, we observed a remarkable epoxidation reaction of a non-activated C=C bond catalyzed by this monooxygenase. Wiley-VCH Verlag GmbH & Co. KGaA, 2008.
Rial, Daniela V.,Bianchi, Dario A.,Kapitanova, Petra,Lengar, Alenka,Van Beilen, Jan B.,Mihovilovic, Marko D.
scheme or table
p. 1203 - 1213
(2009/04/07)
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