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Sci. Pharm.Scientia Pharmaceutica
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  • Scientia Pharmaceutica is published by MDPI from Volume 84 Issue 3 (2016). Previous articles were published by another publisher in Open Access under a CC-BY (or CC-BY-NC-ND) licence, and they are hosted by MDPI on mdpi.com as a courtesy and upon agreement with Austrian Pharmaceutical Society (Österreichische Pharmazeutische Gesellschaft, ÖPhG).
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18 December 2010

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

and
Department of Pharmacy – Center for Drug Research, Ludwig-Maximilians University, Butenandtstr. 5–13, 81377 Munich, Germany
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Sci. Pharm.2011, 79(1), 59-68;https://doi.org/10.3797/scipharm.1011-11
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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.

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