127399-72-8Relevant articles and documents
Synthesis, anti-tubulin and antiproliferative SAR of steroidomimetic dihydroisoquinolinones
Leese, Mathew P.,Jourdan, Fabrice L.,Major, Meriel R.,Dohle, Wolfgang,Thomas, Mark P.,Hamel, Ernest,Ferrandis, Eric,Mahon, Mary F.,Newman, Simon P.,Purohit, Atul,Potter, Barry V. L.
, p. 798 - 812 (2014/05/06)
A SAR translation strategy adopted for the discovery of tetrahydroisoquinolinone (THIQ)-based steroidomimetic microtubule disruptors has been extended to dihydroisoquinolinone (DHIQ)-based compounds. A steroid A,B-ring-mimicking DHIQ core was connected to
ISOQUINOLINE AMINOPYRAZOLE DERIVATIVES, THEIR MANUFACTURE AND USE AS PHARMACEUTICAL AGENTS FOR THE TREATMENT OF CANCER
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Page/Page column 247, (2008/06/13)
Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
Monomethyl Ether Derivatives of 7,8-Dihydroxy- and 8,9-Dihydroxy-4-n-propyl-1,2,3,4,4a,5,6,10b-octahydrobenzoquinolines as Possible Products of Metabolism by Catechol-O-methyltransferase
Cannon, Joseph G.,Walker, Kathleen A.,Montanari, Antonio,Long, John Paul,Flynn, Jan R.
, p. 2000 - 2006 (2007/10/02)
In order to facilitate identification of possible metabolites arising from in vitro action of catechol-O-methyltransferase upon 7,8-dihydroxy- and 8,9-dihydroxy-4-n-propyl-1,2,3,4,4a,5,6,10b-octahydrobenzoquinolines (11, 12), all four possible monomethyl ether derivatives have been synthesized.Incubation of 11 and 12 with the enzyme revealed that the 8,9-dihydroxy positional isomer 12 (which contains the dopamine moiety held in the β conformation) but not the 7,8-dihydroxy isomer 11 (which holds the dopamine moiety in the α conformation) was a substrate for theenzyme.The sole detectable product of 12 was 8-hydroxy-9-methoxy derivative 15 in which the "meta" hydroxy group of the dopamine moiety is etherified.