N-benzoyl-.alpha.-alkylated azatyrosines as anticancer agents

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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546300, A61K 3144, C07D21365

Patent

active

060373571

ABSTRACT:
A series of N-benzoyl-.alpha.-alkylated azatyrosines has been synthesized and disclosed. Their in-vitro activities were positive against several human cancer cell lines and significantly more effective than L-azatyrosine. These azatyrosine derivatives were claimed to be new and be useful as anticancer agents alone or in combination with other anticancer agents. These azatyrosine derivatives may be formulated into suitable pharmaceutical dosage forms for the treatment of cancer.

REFERENCES:
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Junko Fujita-Yoshigaki et al., Azatyrosine inhibits neurite outgrowth of PC12 cells induced by oncogenic Ras, Oncogene (1992) 7, 2019-2024.
Shigeharu Inouye et al., L-.beta.-(5-Hydroxy-2-pyridyl)-alanine and L-.beta.-(3-Hydroxyureido)-alanine from Streptomyces, Chem. Pharm. Bull. 23(11) 2669-2677 (1975).
W. J. Krzyzosiak et al., Isolation of genes specifically expressed in flat revertant cells derived from activated ras-transformed NIH 3T3 cells by treatment with azatyrozine, Proc. Natl. Acad. Sci U.S.A.. 89, 4879-4883, Jun. 1992.
Nobuko Shindo-Okada et al., Permanent Conversion of Mouse and Human Cells Transformed by Activated ras or raf Genes to Apparently Normal Cells by Treatment With the Antibiotic Azatyrosine, Molecular Carcinogenesis 2:159-167 (1989).

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