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The synethesis of a new retinoid, N-(4-hydroxyphenyl)-all-trans-retinamide, which has useful biological properties, is described. This retinoid was more potent than retinyl acetate in reversing keratinization caused by retinoid deficiency in tracheal organ culture. It was markedly less toxic than retinyl acetate when fed p.o. to rats over 2-week or 6-month periods. It was an effective agent for inhibition of the development of breast cancer induced in rats by N-nitroso-N-methylurea, although it was not as potent as retinyl acetate in this regard. However, the lesser toxicity of 4-hydroxyphenylretinamide makes it a superior agent for prevention of breast cancer. High-pressure liquid chromatographic analyses of liver and breast extracts from rats treated for 6 months with retinoids show the pharmacokinetic basis for the superiority of 4-hydroxyphenylretinamide; this retinoid and its metabolites were found in high concentrations in breast tissue, without any measurable accumulation in the liver or evident liver toxicity. In contrast, chronic feeding of retinyl acetate caused marked deposition of retinyl esters in the liver and severe hepatotoxicity. Whole mounts of rat mammary glands, made after chronic feeding of 4-hydroxyphenylretinamide, showed that it had a marked antiproliferative effect on mammary epithelium.
R C Moon, and
H J Thompson, and
P J Becci, and
C J Grubbs, and
R J Gander, and
D L Newton, and
J M Smith, and
S L Phillips, and
W R Henderson, and
L T Mullen, and
C C Brown, and
M B Sporn
October 1995,
Carcinogenesis,
R C Moon, and
H J Thompson, and
P J Becci, and
C J Grubbs, and
R J Gander, and
D L Newton, and
J M Smith, and
S L Phillips, and
W R Henderson, and
L T Mullen, and
C C Brown, and
M B Sporn
December 1999,
Cancer research,
R C Moon, and
H J Thompson, and
P J Becci, and
C J Grubbs, and
R J Gander, and
D L Newton, and
J M Smith, and
S L Phillips, and
W R Henderson, and
L T Mullen, and
C C Brown, and
M B Sporn
November 1994,
International journal of cancer,
R C Moon, and
H J Thompson, and
P J Becci, and
C J Grubbs, and
R J Gander, and
D L Newton, and
J M Smith, and
S L Phillips, and
W R Henderson, and
L T Mullen, and
C C Brown, and
M B Sporn
January 2006,
Journal of experimental therapeutics & oncology,
R C Moon, and
H J Thompson, and
P J Becci, and
C J Grubbs, and
R J Gander, and
D L Newton, and
J M Smith, and
S L Phillips, and
W R Henderson, and
L T Mullen, and
C C Brown, and
M B Sporn
October 1995,
Carcinogenesis,
R C Moon, and
H J Thompson, and
P J Becci, and
C J Grubbs, and
R J Gander, and
D L Newton, and
J M Smith, and
S L Phillips, and
W R Henderson, and
L T Mullen, and
C C Brown, and
M B Sporn
January 1988,
Drug metabolism and disposition: the biological fate of chemicals,
R C Moon, and
H J Thompson, and
P J Becci, and
C J Grubbs, and
R J Gander, and
D L Newton, and
J M Smith, and
S L Phillips, and
W R Henderson, and
L T Mullen, and
C C Brown, and
M B Sporn
October 1996,
Cancer letters,
R C Moon, and
H J Thompson, and
P J Becci, and
C J Grubbs, and
R J Gander, and
D L Newton, and
J M Smith, and
S L Phillips, and
W R Henderson, and
L T Mullen, and
C C Brown, and
M B Sporn
September 2002,
International journal of cancer,
R C Moon, and
H J Thompson, and
P J Becci, and
C J Grubbs, and
R J Gander, and
D L Newton, and
J M Smith, and
S L Phillips, and
W R Henderson, and
L T Mullen, and
C C Brown, and
M B Sporn
June 2010,
The Journal of biological chemistry,
R C Moon, and
H J Thompson, and
P J Becci, and
C J Grubbs, and
R J Gander, and
D L Newton, and
J M Smith, and
S L Phillips, and
W R Henderson, and
L T Mullen, and
C C Brown, and
M B Sporn
December 1988,
The Biochemical journal,
