Miracil D, Its Toxicology, Absorption, and Excretion in Animals and Human Volunteers

Hawking, Frank; Ross, W. Fraser

doi:10.1111/j.1476-5381.1948.tb00370.x

Cited by 6 publications

(2 citation statements)

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“…Thioxanthones are isosteric analogues of xanthones, consisting of S-heterocycles with a dibenzo-γ-thiopyrone scaffold. The first thioxanthone with promising therapeutic value, lucanthone (Miracil D), appeared in the decade of the 1940s as an antischistossomal agent [1,2]. Several studies on the biological activities of thioxanthones allowed their identification as anticancer agents, as well as the identification of their mechanisms of action [2].…”

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confidence: 99%

Screening a Small Library of Xanthones for Antitumor Activity and Identification of a Hit Compound which Induces Apoptosis

et al. 2016

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Our previous work has described a library of thioxanthones designed to have dual activity as P-glycoprotein modulators and antitumor agents. Some of these compounds had shown a significant cell growth inhibitory activity towards leukemia cell lines, without affecting the growth of non-tumor human fibroblasts. However, their effect in cell lines derived from solid tumors has not been previously studied. The present work aimed at: (i) screening this small series of compounds from an in-house library, for their in vitro cell growth inhibitory activity in human tumor cell lines derived from solid tumors; and (ii) initiate a study of the effect of the most potent compound on apoptosis. The tumor cell growth inhibitory effect of 27 compounds was first analysed in different human tumor cell lines, allowing the identification of a hit compound, TXA1. Its hydrochloride salt TXA1¨HCl was then synthesized, to improve solubility and bioavailability. Both TXA1 and TXA1¨HCl inhibited the growth of MCF-7, NCI-H460, A375-C5, HeLa, 786-O, Caki-2 and AGS cell lines. The effect of TXA1¨HCl in MCF-7 cells was found to be irreversible and was associated, at least in part, with an increase in cellular apoptosis.

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Section: Introductionmentioning

confidence: 99%

Screening a Small Library of Xanthones for Antitumor Activity and Identification of a Hit Compound which Induces Apoptosis

et al. 2016

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“…Terms & Conditions of access and use can be found at http:// www.tandfonline.com/page/terms-and-conditions INTRODUCTION Lucanthone (Miracil D) (1) [1][2][3][4] and hycanthone (Etrenol) (2) [5][6][7][8] belong to the thioxanthenone class and have been well known as antischistosomal and anticancer agents. However, Taylor & Francis, our agents, and our licensors make no representations or warranties whatsoever as to the accuracy, completeness, or suitability for any purpose of the Content.…”

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confidence: 99%

One Step Synthesis of N-[1-(2-Diethylamino-ethylamino)-7-(H or methoxy)-9-oxo-9H-thioxanthen-4-ylmethyl]-formamides and, Acetamide from Their Corresponding Alcohols, Hycanthone, and 7-Methoxy-hycanthone

Kwon

2003

Synthetic Communications

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The use of microorganisms for the study of drug metabolism

Clark

McChesney

Hufford

1985

Medicinal Research Reviews

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The potential for the use of microorganisms as tools in the study of drug metabolism appears to be unlimited. The selected examples cited here are only the beginning of what could develop into a widely accepted alternative in vitro model system for studying drug metabolism in humans. As with any other in vitro model system, it is not expected that microbial systems could ever replace animals in biomedical research. The acquisition of data regarding absorption, distribution, and excretion will still require whole animal systems. However, it is clear from the examples cited that microbial systems offer a reliable, reproducible alternative to small animal models for preliminary drug metabolism studies. Due to significant species variation, small animal models may, in many cases, be less reliable than microorganisms as predictive models of human metabolism. It has been estimated that approximately 70 million animals are used each year in the U.S. for biomedical research. The development of any techniques which curtail the sacrifice of such large numbers of animals is welcomed both by animal welfare groups who wish to ensure the humane treatment of laboratory animals and by researchers who additionally appreciate the more practical and economical benefits of such alternatives.

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Miracil D, Its Toxicology, Absorption, and Excretion in Animals and Human Volunteers

Cited by 6 publications

References 1 publication

Screening a Small Library of Xanthones for Antitumor Activity and Identification of a Hit Compound which Induces Apoptosis

Screening a Small Library of Xanthones for Antitumor Activity and Identification of a Hit Compound which Induces Apoptosis

One Step Synthesis of N-[1-(2-Diethylamino-ethylamino)-7-(H or methoxy)-9-oxo-9H-thioxanthen-4-ylmethyl]-formamides and, Acetamide from Their Corresponding Alcohols, Hycanthone, and 7-Methoxy-hycanthone

The use of microorganisms for the study of drug metabolism

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