Griseofulvin was identified as an inhibitor of centrosomal clustering in a recently developed assay. Centrosomal clustering is an important cellular event that enables bipolar mitosis for cancer cell lines harboring supernumerary centrosomes. We report herein the synthesis and SAR of 34 griseofulvin analogues as inhibitors of centrosomal clustering. The variations in the griseofulvin structure ...

A rapid and accurate method is described for the determination of griseofulvin and dechlorogriseofulvin extracted from Penicillium urticae with chloroform. Thinlayer chromatography was used to tentatively identify griseofulvin or dechlorogriseofulvin, or both. Two gas-liquid chromatographic systems provided additional qualitative information and simultaneous quantitation of the individual compo...

Because of the interest in Griseofulvin in respect to its fungicidal properties, it was felt that it would be useful to undertake a very l i mited prel iminary trial in order to ascerta in whether Griseofulvin has any effect on the M. leprae. Early workers, particularly REEN­ STIERNA, was of the opinion that M. leprae was originally a so i l fungus and, over the centuries, adapted itself to hu ...

We developed an extensive yeast gene expression library consisting of full-genome cDNA array data for over 500 yeast strains, each with a single-gene disruption. Using this data, combined with dose and time course expression experiments with the oral antifungal agent griseofulvin, whose exact molecular targets were previously unknown, we used Boolean and Bayesian network discovery techniques to...

Oral ketoconazole was recently the subject of regulatory safety warnings because of its association with increased risk of inducing hepatic injury. However, the relative hepatotoxicity of antifungal agents has not been clearly established. The aim of this study was to compare the hepatotoxicity induced by five commonly prescribed oral antifungal agents. Rats were treated with therapeutic oral d...

Background : Dermatophytosis is the common cutaneous infections in humans and animals, which is caused by the keratinophylic fungus called dermatophytes. In recent years , drug-resistance in pathogenic fungi, including dermatophytes to the current antifungal have been increased . The aim of this study was to evaluate the antifungal efficacy of AgNPs against Microsporum canis, Trichophyton menta...

A simple, specific, sensitive, and rapid high performance liquid chromatography (HPLC) method for the determination of griseofulvin in small volumes of rat plasma was developed and validated using warfarin as an internal standard. Biological sample preparation involved simple extraction with acetonitrile, followed by dilution with aqueous mobile phase buffer (20 mM sodium dihydrogen phosphate, ...

INTRODUCTION Gemcitabine is a pyrimidine nucleoside analog that becomes triphosphorylated and in this form it competitively inhibits cytidine incorporation into DNA strands. Diphosphorylated gemcitabine irreversibly inhibits ribonucleotide reductase thereby preventing deoxyribonucleotide synthesis. Functioning as a potent chemotherapeutic, gemcitabine decreases neoplastic cell proliferation and...

Griseofulvin, an antifungic metabolite produced by several species of Penicillium [ 1 ] , is widely used in human and animal therapy [2]. Its mechanism of action remained puzzling for along time [3]. Recently it has been shown that griseofulvin inhibits the polymerization of purified brain tubulin [4,5]. Although this property may account for its in vivo effects, this result does not allow to r...