2. Academic Validation
  3. Synthesis and antiplasmodial activity of aminoalkylamino-substituted neocryptolepine derivatives

Synthesis and antiplasmodial activity of aminoalkylamino-substituted neocryptolepine derivatives

  • J Med Chem. 2009 May 14;52(9):2979-88. doi: 10.1021/jm801490z.
Ibrahim El Sayed 1,  Pieter Van der Veken,  Koen Steert,  Liene Dhooghe,  Steven Hostyn,  Gitte Van Baelen,  Guy Lemière,  Bert U W Maes,  Paul Cos,  Louis Maes,  Jurgen Joossens,  Achiel Haemers,  Luc Pieters,  Koen Augustyns
Affiliations

Affiliation

  • 1 Laboratory of Medicinal Chemistry, University of Antwerp, Universiteitsplein, 1, 2610, Antwerp, Belgium.
PMID: 19364118 DOI: 10.1021/jm801490z
Abstract

A series of chloro- and aminoalkylamino-substituted neocryptolepine (5-methyl-5H-indolo[2,3-b]quinoline) derivatives were synthesized and evaluated as antiplasmodial agents. The evaluation also included cytotoxicity (MRC5 cells), inhibition of beta-hematin formation, and DNA interactions (DNA-methyl green assay). Introduction of aminoalkylamino chains increased the antiplasmodial activity of the neocryptolepine core substantially. The most efficient compounds showed antiplasmodial activities in the nanomolar range. N(1),N(1)-Diethyl-N(4)-(5-methyl-5H-indolo[2,3-b]quinolin-8-yl)pentane-1,4-diamine 11c showed an IC(50) of 0.01 microM and a selectivity index of 1800.

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