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Synthesis and Antitumor Activity of 1,5-Disubstituted 1,2,4-Triazoles as Cis-Restricted Combretastatin Analogues

  1. Author:
    Romagnoli, R.
    Baraldi, P. G.
    Cruz-Lopez, O.
    Cara, C. L.
    Carrion, M. D.
    Brancale, A.
    Hamel, E.
    Chen, L. C.
    Bortolozzi, R.
    Basso, G.
    Viola, G.

  2. Author Address

    [Romagnoli, Romeo; Baraldi, Pier Giovanni; Cruz-Lopez, Olga; Cara, Carlota Lopez; Carrion, Maria Dora] Univ Ferrara, Dipartimento Sci Farmaceut, I-44100 Ferrara, Italy. [Brancale, Andrea] Cardiff Univ, Welsh Sch Pharm, Cardiff CF10 3NB, S Glam, Wales. [Hamel, Ernest] NCI, Screening Technol Branch, Dev Therapeut Program, Div Canc Treatment & Diag,NIH, Frederick, MD 21702 USA. [Chen, Longchuan] VA Med Ctr, Dept Pathol, Long Beach, CA 90822 USA. [Bortolozzi, Roberta; Basso, Giuseppe; Viola, Giampietro] Univ Padua, Dipartimento Pediat, Lab Oncoematol, I-35131 Padua, Italy.;Romagnoli, R, Univ Ferrara, Dipartimento Sci Farmaceut, I-44100 Ferrara, Italy.;rmr@unife.it giampietro.viola1@unipd.it
    1. Year: 2010
    2. Date: May
  2. Journal: Journal of Medicinal Chemistry
    1. 53
    2. 10
    3. Pages: 4248-4258
  4. Type of Article: Article
  5. ISSN: 0022-2623
  1. Abstract:

    A series of 1-aryl-5-(3',4',5'-trimethoxyphenyl) derivatives and their related 1-(3',4',5'-trimethoxyphenyl)5-aryl-1,2,4-triazoles, designed as cis-restricted combretastatin analogues, were synthesized and evaluated for antiproliferative activity, inhibitory effects on tubulin polymerization, cell cycle effects, and apoptosis induction. Their activity was greater than, or comparable with, that of the reference compound CA-4. Flow cytometry studies showed that HeLa and Jurkat cells treated with the most active compounds 4l and 4o were arrested in the G2/M phase of the cell cycle in a concentration dependent manner. This effect was accompanied by apoptosis of the cells, mitochondrial depolarization, generation of reactive oxygen species, activation of caspase-3, and PA RP cleavage. Compound 41 was also shown to have potential antivascular activity, since it induced endothelial cell shape change in vitro and disrupted the sprouting of endothelial cells in the chick aortic ring assay.

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External Sources

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  2. DOI: 10.1021/jm100245q
  3. View record in Web of Science®
  4. WOS: 000277766900035

Library Notes

  1. Fiscal Year: FY2009-2010
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