2-(4-Aminophenyl)benzothiazoles display potent and selective antitumor activity against inter alia breast, ovarian, colon, and renal cell lines, but their mechanism of action, though yet to be defined, may be novel. Metabolism is suspected to play a central role in the mode of action of these benzothiazoles since drug uptake and biotransformation were observed in sensitive cell lines (e.g., breast MCF-7 and MDA 468 cells) in vitro, whereas insensitive cell lines (e.g., prostate PC 3 cells) showed negligible uptake and biotransformation. N-Acyl derivatives of the arylamines have been synthesized, and in vitro studies confirm N-acetylation and oxidation as the main metabolic transformations of 2-(4-aminophenyl)benzothiazoles, with the predominant process being dictated by the nature of the 3'-substituent. The prototype amine 3 underwent mainly N-acetylation in vitro, while 3'-substituted analogues 4 and 5 were primarily oxidized. N-Acetylation of 4 to 11 exerts a drastic dyschemotherapeutic effect in vitro, but acetylation of the halogeno congeners 5-7 gave acetylamines 12-14 which substantially retain selective antitumor activity. In vivo pharmacokinetic studies in rats confirmed rapid and exclusive N-acetylation of the 3'-methyl analogue 4, but less acetylation with the 3'-chloro analogue 5. Distinct expression patterns of N-acetyltransferase NAT1 and NAT2 have been demonstrated in our panel of cell lines.
ObjectiveTo understand how the formal curriculum experience of an Australian
undergraduate pharmacy program supports students’ professional identity
formation.MethodsA qualitative ethnographic study was conducted over four weeks using
participant observation and examined the ‘typical’ student experience from
the perspective of a pharmacist. A one-week period of observation was
undertaken with each of the four year groups (that is, for years one to
four) comprising the undergraduate curriculum. Data were collected through
observation of the formal curriculum experience using field notes, a
reflective journal and informal interviews with 38 pharmacy students. Data
were analyzed thematically using an a priori analytical framework.ResultsOur findings showed that the observed curriculum was a conventional
curricular experience which focused on the provision of technical knowledge
and provided some opportunities for practical engagement. There were some
opportunities for students to imagine themselves as pharmacists, for
example, when the lecture content related to practice or teaching staff
described their approach to practice problems. However, there were limited
opportunities for students to observe pharmacist role models, experiment
with being a pharmacist or evaluate their professional identities. While
curricular learning activities were available for students to develop as
pharmacists e.g. patient counseling, there was no contact with patients and
pharmacist academic staff tended to role model as educators with little
evidence of their pharmacist selves.ConclusionsThese findings suggest that the current conventional approach to the
curriculum design may not be fully enabling learning experiences which
support students in successfully negotiating their professional identities.
Instead it appeared to reinforce their identities as students with a naïve
understanding of professional practice, making their future transition to
professional practice challenging.
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