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Sci. Pharm. 2011, 79(1), 59-68; doi:10.3797/scipharm.1011-11

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

Department of Pharmacy – Center for Drug Research, Ludwig-Maximilians University, Butenandtstr. 5–13, 81377 Munich, Germany
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Author to whom correspondence should be addressed.
Received: 30 November 2010 / Accepted: 17 December 2010 / Published: 18 December 2010
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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.
Keywords: gamma-Carboline; Gramine; Lactam; Cytotoxic activity; Antifungal activity gamma-Carboline; Gramine; Lactam; Cytotoxic activity; Antifungal activity
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

WOLLEIN, U.; BRACHER, F. The Gramine Route to Pyrido[4,3-b]indol-3-ones – Identification of a New Cytotoxic Lead. Sci. Pharm. 2011, 79, 59-68.

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