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Synthesis of Triazenoazaindoles: a New Class of Triazenes with Antitumor Activity

✍ Scribed by Prof. Patrizia Diana; Dr. Antonina Stagno; Prof. Paola Barraja; Dr. Anna Carbone; Dr. Barbara Parrino; Prof. Francesco Dall'Acqua; Prof. Daniela Vedaldi; Dr. Alessia Salvador; Dr. Paola Brun; Prof. Ignazio Castagliuolo; Prof. Olaf Georg Issinger; Prof. Girolamo Cirrincione

Publisher
John Wiley and Sons
Year
2011
Tongue
English
Weight
435 KB
Volume
6
Category
Article
ISSN
1860-7179

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✦ Synopsis

Abstract

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 μM) 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.

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## Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.