The central role of iron in tumor progression and metastasis motivates the development of iron-binding approaches in cancer chemotherapy. Disulfide-based prochelators are reductively activated upon cellular uptake to liberate thiol chelators responsible for iron sequestration. Herein, a trimethyl thiosemicarbazone moiety and the imidazole-2-thione heterocycle are incorporated in this prochelator design.
View Article and Find Full Text PDFTridentate aroyl hydrazones are effective metal chelators in biological settings, and their activity has been investigated extensively for medicinal applications in metal overload, cancer, and neurodegenerative diseases. The aroyl hydrazone motif is found in the recently reported prochelator (AH1-S), which has shown antiproliferative proapoptotic activity in mammalian cancer cell lines. Intracellular reduction of this disulfide prochelator leads to the formation of mercaptobenzaldehyde benzoylhydrazone chelator AH1 and to iron sequestration, which in turn impacts cell growth.
View Article and Find Full Text PDFThe iron metabolism of malignant cells, which is altered to ensure higher acquisition and utilization, motivates the investigation of iron chelation strategies in cancer treatment. In a prochelation approach aimed at increasing intracellular specificity, disulfide reduction/activation switches are incorporated on iron-binding scaffolds resulting in intracellularly activated scavengers. Herein, this strategy is applied to several tridentate donor sets including thiosemicarbazones, aroylhydrazones and semicarbazones.
View Article and Find Full Text PDFJ Dermatolog Treat
September 2004
Background: Erythromycin is a common therapy for acne and rosacea. A newer macrolide, azithromycin, offers superior tissue distribution and cellular concentration and is an effective oral anti-acne agent. Topical formulations such as erythromycin have been a major clinical therapy for acne.
View Article and Find Full Text PDFBull Med Libr Assoc
July 1974
To illustrate the extent of time lags from manuscript submission to journal publication certain "core" journals in neurology and general medicine have been surveyed. The clinical journals experience less time lag, but more of a problem with backlogs of manuscripts, than basic research journals. Most editors of the journals surveyed cited the following as the major causes for publication delay: failure of authors to follow journal requirements, slowness of editorial and referee reviews, and author revisions.
View Article and Find Full Text PDFNo abnormality of exocrine function of the pancreas was found in 10 patients with amyotrophic lateral sclerosis. Eight patients showed abnormal glucose metabolism, attributed to the effects of age, malnutrition, diminished physical activity, and decreased muscle mass.
View Article and Find Full Text PDFJ Neurol Neurosurg Psychiatry
August 1969