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Synthesis of Triazenoazaindoles: a New Class of Triazenes with Antitumor Activity
Author(s) -
Diana Patrizia,
Stagno Antonina,
Barraja Paola,
Carbone Anna,
Parrino Barbara,
Dall'Acqua Francesco,
Vedaldi Daniela,
Salvador Alessia,
Brun Paola,
Castagliuolo Ignazio,
Issinger Olaf Georg,
Cirrincione Girolamo
Publication year - 2011
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201100027
Subject(s) - cytotoxicity , dacarbazine , apoptosis , melanoma , cell culture , cancer research , flow cytometry , leukemia , programmed cell death , chemistry , cancer cell , cancer , pharmacology , biology , biochemistry , microbiology and biotechnology , in vitro , immunology , genetics
Despite improvements in the treatment and prevention of cancer, the number of new diagnoses continues to rise; this has fuelled substantial interest in the development of new and effective chemotherapeutic agents. Compounds of the triazene class, such as dacarbazine, have been used in the clinical management of many cancer types including brain, leukemia, and melanoma. A new compound class bearing a triazenoazaindole scaffold was synthesized with the aim of identifying new antiproliferative agents. Compounds 5 a – g and 6 a – c were screened against a panel of human tumor cell lines, and two of them, 5 e and 5 f , showed cytotoxicity (GI 50 range: 2.2–8.2 μ M ) in all cell lines. These two compounds even maintained their cytotoxicity in some multidrug‐resistant cell lines. Flow cytometry analysis demonstrated their ability to induce cell death by apoptosis with involvement of lysosomes.