34206-49-0Relevant articles and documents
Synthesis and biological activity of 10-aza-narciclasine
Vshyvenko, Sergey,W'Giorgis, Zemane,Weber, Audrey,Neverova, Natalia,Hedberg, Bradley,Hudlicky, Tomas
, p. 83 - 87 (2015)
The first active aza analogue of narciclasine was synthesized from a pentasubstituted derivative of nicotinic acid. The key features of the synthesis include a halogen dance of bromopyridine and an intramolecular Heck reaction with a conduramine derived chemoenzymatically from bromobenzene. 10-Aza-narciclasine was found to have reasonable activity against several cancer cell lines.
Indoline -1H- pyrazolo [3,4-d] pyrimidinone compound, as well as preparation method and application thereof
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Paragraph 0162-0165, (2020/03/17)
The present invention relates to a compound of Formula (I), or a pharmaceutically acceptable salt, thereof, which may be better selective Wee1 as a new generation, selective inhibitor Wee1 with respect to the existing, inhibitor Wee1 for, Kinase more safe
NITROGEN-CONTAINING BICYCLIC HETEROCYCLES FOR USE AS ANTIBACTERIALS
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Page/Page column 62, (2010/02/07)
Cyclohexane and cyclohexene derivatives and pharmaceutically acceptable derivatives hereof useful in methods of treatment of bacterial infections in mammals, particularly man.
Inactivation of O6-alkylguanine-DNA alkyltransferase. 1. Novel O6-(hetarylmethyl)guanines having basic rings in the side chain.
McElhinney,Donnelly,McCormick,Kelly,Watson,Rafferty,Elder,Middleton,Willington,McMurry,Margison
, p. 5265 - 5271 (2007/10/03)
A number of novel guanine derivatives containing heterocyclic moieties at the O6-position have been synthesized using a purine quaternary salt which reacts with alkoxides under mild conditions. Initially O6-substituents were investigated in which the benzene ring of the known agent, O6-benzylguanine, was replaced by unsubstituted heterocyclic rings. The ability of these agents to inactivate the DNA repair protein O6-alkylguanine-DNA alkyltransferase (ATase), both as pure recombinant protein and in the human lymphoblastoid cell line Raji, has been compared with that of O6-benzylguanine. The present paper focuses on O6-substituents with basic rings, and under standard conditions several of them proved more effective than benzyl for inactivation of both recombinant and Raji ATase. Among the pyridine derivatives, the 2-picolyl compound 7 is not very active in contrast to the 3- and 4-picolyl compounds, and this influenced our choice of isomers of other basic ring systems for study. Since halogen substitution in the thiophene ring considerably increased the activity (17 versus 6), similar modifications in the pyridine series were examined. The more polar O6-substituents in this study are on the whole compatible with the stereochemical requirements of the ATase protein, and their pharmacological properties may be valuable in subsequent in vivo investigations, particularly the thenyl (6), 5-thiazolylmethyl (12), 5-bromothenyl (17), and 2-chloro-4-picolyl (21) derivatives.