Regioselective Synthesis of Pyrazolo[4, 5-g]pyrido[1, 2-a]benzimidazoles : Cytotoxic Derivatives of Pyrido[1, 2-a]benzimidazolic Ring System

Marianne DUPUY; Frederic PINGIET; Yves BLACHE; Olivier CHAVIGNON; Jean-Claude TEULADE; Jean-Pierre CHAPAT

doi:10.1248/cpb.46.1820

Marianne DUPUY, Frederic PINGIET, Yves BLACHE, Olivier CHAVIGNON, Jean-Claude TEULADE, Jean-Pierre CHAPAT

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Keywords: pyrazolo[4, 5-g]pyrido[1, 2-a]benzimidazole, pyrido[1, 2-a]benzimidazole, pyrazole, anticancer agents, multidrug resistance, glycoprotein GP 170

JOURNAL FREE ACCESS

1998 Volume 46 Issue 11 Pages 1820-1823

DOI https://doi.org/10.1248/cpb.46.1820

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Abstract

N-1 and N-2 substituted pyrazolo[4, 5-g]pyrido[1, 2-a]benzimidazoles were prepared regioselectively, and cytotoxicities evaluated in vitro against K562 and HL60 cells. All compounds displayed weaker activity than doxorubicin against sensitive lines, but showed the same activity against resistant cell lines (multidrug resistance +, (MDR⁺); K562R and HL60R) indicating no resistance phenomena.

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