The publication detail shows the title, authors (with indicators showing other profiled authors), information on the publishing organization, abstract and a link to the article in PubMed. This abstract is what is used to create the fingerprint of the publication. If any grants are referenced by the publication, they will be listed here as well.
In vitro evaluation of amino acid prodrugs of novel antitumour 2-(4-amino-3-methylphenyl)benzothiazoles.
T D Bradshaw; M-S Chua; H L Browne; V Trapani; E A Sausville; M F G Stevens (Profiled Author: Edward A Sausville)
Cancer Research Laboratories, School of Pharmaceutical Sciences, University of Nottingham, Nottingham NG7 2RD, UK. firstname.lastname@example.org
British journal of cancer 2002;86(8):1348-54.
Novel 2-(4-aminophenyl)benzothiazoles possess highly selective, potent antitumour properties in vitro and in vivo. They induce and are biotransformed by cytochrome P450 (CYP) 1A1 to putative active as well as inactive metabolites. Metabolic inactivation of the molecule has been thwarted by isosteric replacement of hydrogen with fluorine atoms at positions around the benzothiazole nucleus. The lipophilicity of these compounds presents limitations for drug formulation and bioavailability. To overcome this problem, water soluble prodrugs have been synthesised by conjugation of alanyl- and lysyl-amide hydrochloride salts to the exocyclic primary amine function of 2-(4-aminophenyl)benzothiazoles. The prodrugs retain selectivity with significant in vitro growth inhibitory potency against the same sensitive cell lines as their parent amine, but are inactive against cell lines inherently resistant to 2-(4-aminophenyl)benzothiazoles. Alanyl and lysyl prodrugs rapidly and quantitatively revert to their parent amine in sensitive and insensitive cell lines in vitro. Liberated parent compounds are sequestered and metabolised by sensitive cells only; similarly, CYP1A1 activity and protein expression are selectively induced in sensitive carcinoma cells. Amino acid prodrugs meet the criteria of aqueous solubility, chemical stability and quantitative reversion to parent molecule, and thus are suitable for in vivo preclinical evaluation.
This section shows information related to the publication - computed using the fingerprint of the publication - including related publications, related experts and related grants with fingerprints representing significant amounts of overlap between their fingerprint and this publication. The red dots indicate whether those experts or terms appear within the publication, thereby showing potential and actual connections.
Tracey D Bradshaw; Michael C Bibby; John A Double; Iduna Fichtner; Patricia A Cooper; Michael C Alley; Susan Donohue; Sherman F Stinson; Joseph E Tomaszewjski; Edward A Sausville; et al.Molecular cancer therapeutics 2002;1(4):239-46.
M S Chua; E Kashiyama; T D Bradshaw; S F Stinson; E Brantley; E A Sausville; M F StevensCancer research 2000;60(18):5196-203.
Andrea I Loaiza-Pérez; Valentina Trapani; Curtis Hose; Sheo S Singh; Jane B Trepel; Malcolm F G Stevens; Tracey D Bradshaw; Edward A SausvilleMolecular pharmacology 2002;61(1):13-9.
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