91281-33-3Relevant academic research and scientific papers
Biomimetic Oxidation of the Antimelanoma Agent 4-S-Cysteaminylphenol and Related Catechol Thioethers: Isolation and Reaction Behaviour of Novel Dihydrobenzothiazinequinones
Mascagna, Donatella,Costantini, Claudio,d'Ischia, Marco,Prota, Giuseppe
, p. 8757 - 8764 (1994)
Enzymatic and chemical oxidation of 4-S-cysteaminylphenol (1) and 4-S-cysteaminylcatechol (2) leads to the formation of the hitherto unknown dihydrobenzothiazine-6,7-quinone 4 via intramolecular cyclisation of the o-quinone 6.Oxidation of 4-S-cysteinylcat
Phenylethylamine derivatives and their use in the treatment of melanoma
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, (2008/06/13)
Novel mono- and dihydroxy phenylethylamine derivatives useful in treating melanoma are provided having the formulae (Ia, Ib or Ic). In the above formulae, Ra is hydrogen or —COORb, Rb is hydrogen or C1-6 alkyl;
Melanocyte-directed enzyme prodrug therapy (MDEPT): Development of second generation prodrugs for targeted treatment of malignant melanoma
Jordan, Allan M.,Khan, Tariq H.,Malkin, Hugh,Osborn, Helen M.I.,Photiou, Andrew,Riley, Patrick A.
, p. 1549 - 1558 (2007/10/03)
Evaluation of second generation prodrugs for MDEPT, by oximetry, has highlighted structural properties that are advantageous and disadvantageous for efficient oxidation using mushroom tyrosinase. In particular, a sterically undemanding prodrug bis-(2-chlo
Antihypertensive activities of phenyl aminoethyl sulfides, a class of synthetic substrates for dopamine β-hydroxylase
Padgette,Herman,Hee Han,et al.
, p. 1354 - 1357 (2007/10/02)
Four sulfur-containing analogues of phenylpropylamine were synthesized and evaluated as substrates for dopamine β-hydroxylase (DBH) and monoamine oxidase (MAO). All four phenyl aminoethyl sulfides were shown to be good substrates for DBH whereas only the two analogues not possessing a methyl group α to the terminal amino group were substrates for MAO. All four analogues were tested for acute antihypertensive activity in an animal model for hypertension, the spontaneously hypertensive rat (SHR). Two of the analogues, both of which should partition readily across the blood-brain barrier, did not appreciably reduce systemic blood pressure in the 6-h testing period. However, the two analogues that were designed to be relatively restricted to peripheral sites of action caused a dramatic drop in blood pressure in SHR of 25% within 1-1.5-h postinjection, with the analogue designed to be both restricted to the periphery and MAO inactive, causing a more prolonged antihypertensive activity.
