Sulfur Analogues of Tyrosine in the Development of Triazene Hybrid Compounds: A New Strategy against Melanoma.

ABSTRACT: Malignant melanoma is the major cause of death from skin cancer. Treatment of metastatic melanoma remains an enormous challenge. In this study we developed hybrid compounds and studied their potential use in malignant melanoma chemotherapy. They were designed to act by a double mechanism of action, being composed of two pharmacophores: the tyrosine sulfur analogue 4-S-cysteaminylphenol (4-S-CAP, 10), with immunomodulatory properties and specific melanocytotoxic activity, and triazene 4, with DNA alkylating properties. The design of these compounds aims to achieve selective activation by the enzyme tyrosinase overexpressed in melanoma cells. Compounds 11a-e, 13a, and 13b were found to be excellent tyrosinase substrates (0.5 min ≤ t

SUBMITTER: Granada M 

PROVIDER: S-EPMC8591744 | biostudies-literature | 2021 Nov

REPOSITORIES: biostudies-literature