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Synthesis and cytostatic activity of new 1-substituted 6H-pyrido[4,3-b]carbazole derivatives

Beata Tylińska 1Ryszard Jasztold-Howorko 1Beata Filip-Psurska 2Dagmara B. Kłopotowska 2Joanna Wietrzyk 2

1. Wrocław Medical University, Faculty of Pharmacy, Department of Organic Chemistry, Grodzka 9, Wrocław 50-137, Poland
2. Polish Academy of Sciences, Institute of Immunology and Experimental Therapy (IITD), Rudolfa Weigla 12, Wrocław 53-114, Poland


Olivacine 1 is a natural alkaloid isolated from the bark and stem of Aspidosperma olivaceum Müll. Arg. [1], which exhibits anticancer activity. 1,5-Dimethyl-6H-pyrido[4,3-b]carbazole 1 is an intercalating compound and has high DNA binding affinity, which is responsible for its pharmacological properties.

Based on the literature data and on our personal results of research [2-4] we have designed the syntheses of some new 1-substituted pyrido[4,3-b]carbazole derivatives. Presented paper described the synthesis and antitumor activity of some new 1-phenyl 9-hydroxy(or methoxy) 6H-pyrido[4,3-b]carbazole derivatives 2.

Cytostatic activity of these compounds was performed in the Institute of Immunology and Experimental Therapy Wrocław Poland.

[1] J. Schmutz, F. Hunzicker, Pharm. Acta Helv., 1958, 30, 341-347.
[2] C. Landras, R. Jasztold-Howorko, A. Pierré, S. Léonce, N. Guilbaud, L. Kraus-Berthier, C. Guillonneau, Y. Rolland, G. Atassi, E. Bisagni. Chem. Pharm. Bull. 1996, 44, 2169-2172.
[3] R. Jasztold-Howorko, A. Croisy, D. Carrez, I. Jaroszewicz, A. Nasulewicz, M. Pełczyńska, A. Opolski, Arch. Pharm. Med. Chem. 2004, 337, 599-604.
[4] R. Jasztold-Howorko, M. Pełczyńska, A. Nasulewicz, J. Wietrzyk, A. Opolski, Arch. Pharm. Chem. Life Sci. 2005, 338, 556-561.


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Presentation: Poster at VI Multidyscyplinarna Konferencja Nauki o Leku, by Beata Tylińska
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Submitted: 2008-03-12 11:43
Revised:   2009-06-07 00:48