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Scientia Pharmaceutica
Year: 2011  |  Volume: 79  |  Issue: 1  |  Page No.: 59 - 68

The Gramine Route to Pyrido[4,3-b]indol-3-ones -Identification of a New Cytotoxic Lead

Uwe WOLLEIN and Franz BRACHER    

Abstract: A novel approach to 3-oxo-γ-carbolines was worked out starting from methyl indol-2-ylacetate via a gramine derivative. After quaternization, ammonia and 4-methoxybenzylamine could be inserted giving appropriate 3-oxo-γ-carbolines. Condensation with 2-chlorobenzaldehyde under microwave irradiation gave a 4-(2-chlorobenzyl)-3-oxo-γ-carboline. N-methylation lead to a product with very promising antifungal and cytotoxic activities. Keywords

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