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Synthesis and in vitro Evaluation of 3H-Pyrrolo[3,2-f]quinolin-9-one Derivatives That Show Potent and Selective Anti-leukemic Activity

  1. Author:
    Ferlin, M. G.
    Bortolozzi, R.
    Brun, P.
    Castagliuolo, I.
    Hamel, E.
    Basso, G.
    Viola, G.

  2. Author Address

    [Ferlin, Maria Grazia] Univ Padua, Dept Pharmaceut Sci, Fac Pharm, I-35131 Padua, Italy. [Bortolozzi, Roberta; Basso, Giuseppe; Viola, Giampietro] Univ Padua, Dept Pediat, Lab Oncohematol, I-35131 Padua, Italy. [Brun, Paola; Castagliuolo, Ignazio] Univ Padua, Dept Histol Microbiol & Med Biotechnol, I-35131 Padua, Italy. [Hamel, Ernest] NCI, Screening Technol Branch, Dev Therapeut Program, Div Canc Treatment & Diag,NIH, Frederick, MD 21702 USA.;Ferlin, MG, Univ Padua, Dept Pharmaceut Sci, Fac Pharm, Via Marzolo 5, I-35131 Padua, Italy.;mariagrazia.ferlin@unipd.it
    1. Year: 2010
    2. Date: Jul
  2. Journal: Chemmedchem
    1. 5
    2. 8
    3. Pages: 1373-1385
  4. Type of Article: Article
  5. ISSN: 1860-7179
  1. Abstract:

    A series of new substituted 7-phenyl-3H-pyrrolo[3,2-f]quinolin-9-ones were synthesized and evaluated for their antiproliferative activity. The most active derivatives showed high selectivity against human leukemia cell lines and potently inhibited their growth, with GI(50) values in the nanomolar range. The active compounds strongly blocked tubulin assembly and colchicine binding to tubulin. Their activities were equal to or greater than that of the reference compound combretastatin A-4. Flow cytometry studies showed that the two most active compounds arrested Jurkat cells in the G(2)/M cell-cycle phase in a concentration-dependent manner. This effect was associated with apoptosis, mitochondrial depolarization, generation of reactive oxygen species, activation of caspase-3, and cleavage of the enzyme poly(ADP-ribose) polymerase.

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External Sources

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  2. DOI: 10.1002/cmdc.201000180
  3. View record in Web of Science®
  4. WOS: 000281061300022

Library Notes

  1. Fiscal Year: FY2009-2010
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