Method of inhibiting lung tumors, arylalkyl isothiocyanates, and

Details Method of inhibiting lung tumors, arylalkyl isothiocyanates, and Method of inhibiting lung tumors, arylalkyl isothiocyanates, and

1990-05-31

1992-05-19

Goldberg, Jerome D.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Ester doai

A61K 3121, A61K 3126

Patent

active

051149699

ABSTRACT:
A method of inhibiting lung tumor multiplicity and/or incidence by treating mammals with relatively long chain arylalkyl isothiocyanates, especially effective with respect to tumors induced by exposure to tobacco-specific nitrosamine. Among the isothiocyanates are 4-phenylbutyl isothiocyanate, phenylpentyl isothiocyanate and phenylhexyl isothiocyanate, which are synthesized by adding hydrochloride of phenylbutylamine, phenylpentylamine, or phenylhexylamine in water to thiophosgene in an inert organic solvent. For comparison testing, oxo-pyridyl butyl isothiocyanate is synthesized by dissolving myosmine in HCl to obtain a hydrochloride salt, suspending the salt in dry chloroform, adding thiophosgene, and adding chloroform containing triethylamine.

REFERENCES:
Chemical Abstracts 102:214760w (1985).
Chemical Abstracts 110:88164e (Mar. 13, 1989).
Fung-Lung Chung, Minyao Wang, and Stephen S. Hecht; "Effects of Dietary Indoles and Isothiocyanates on N-Nitrosodimethylamine and 4-(Methylnitrosamino-1-(3-Pyridyl)1-Butanone .alpha.-Hydroxylation and DNA Methylation In Rat Liver"; Carcinogenesis; vol. 6, No. 4, pp. 539-543, 1985.
Effects of alkyl chain length on the inhibition of NNK-induced lung neoplasia in A/J mice by arylalkyl isothiocyanates Carcinogensis vol. 10, No. 9, pp. 1757-1759, 1989.
Inhibition of 4-(Methylnitrosamino)-1-(3-pyridyl)-1-butanone-induced DNA Adduct Formation and Tumorigenicity in the Lung of F344 Rats by Dietary Phenethyl Isothiocyanate Cancer Research 49, 549-533, Feb. 1, 1989.
Effects of Aromatic Isothiocyantes on Tumorigenicity, O.sup.6 -Methylguanine Formation, and Metabolism of the Tobacco-specific Nitrosamine 4-(Methylnitrosamino)-1-(3-pyridyl)-1-butanone in A/J Mouse Lung Cancer Research 49, 2894-2897, Jun. 1, 1989.

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