Display options
Cite
Giansanti V, Piscitelli F, Camboni T, et al. Arylthioindoles: Promising compounds against cancer cell proliferation. Oncol Lett. 2010;1(1):109-112doi: 10.3892/ol_00000020.
Giansanti, V., Piscitelli, F., Camboni, T., Prosperi, E., LA Regina, G., Parks, M., Silvestri, R., & Scovassi, A. I. (2010). Arylthioindoles: Promising compounds against cancer cell proliferation. Oncology letters, 1(1), 109-112. https://doi.org/10.3892/ol_00000020
Giansanti, Vincenzo, et al. "Arylthioindoles: Promising compounds against cancer cell proliferation." Oncology letters vol. 1,1 (2010): 109-112. doi: https://doi.org/10.3892/ol_00000020
Giansanti V, Piscitelli F, Camboni T, Prosperi E, LA Regina G, Parks M, Silvestri R, Scovassi AI. Arylthioindoles: Promising compounds against cancer cell proliferation. Oncol Lett. 2010 Jan;1(1):109-112. doi: 10.3892/ol_00000020. Epub 2010 Jan 01. PMID: 22966266; PMCID: PMC3436460.
Copy Download .nbib Format: NLM
Share it on

Oncol Lett. 2010 Jan;1(1):109-112. doi: 10.3892/ol_00000020. Epub 2010 Jan 01.

Arylthioindoles: Promising compounds against cancer cell proliferation.

Oncology letters

Vincenzo Giansanti, Francesco Piscitelli, Tania Camboni, Ennio Prosperi, Giuseppe LA Regina, Michele Parks, Romano Silvestri, Anna Ivana Scovassi

Affiliations

  1. Istituto di Genetica Molecolare CNR, 27100 Pavia.

PMID: 22966266 PMCID: PMC3436460 DOI: 10.3892/ol_00000020

Abstract

Drugs that are able to modulate the microtubule dynamics either by inhibiting tubulin polymerization or by blocking microtubule disassembly are of great interest in anti-cancer therapy; a number of them are currently applied in clinical development. Tubulin polymerization inhibitors, including arylthioindoles, are characterized by the presence of an indole nucleus and have been obtained from natural sources or prepared by semi-synthesis. We characterized the effect of 5-bromo-3-[(3,4,5-trimetoxyphenyl)thio]-1H-indole (RS 2518) on the metabolism of human cell lines derived from solid tumors. We found that this new compound impairs cell adhesion, arrests the cells in the G(2)/M cell cycle phase and inhibits cell proliferation, thus leading to apoptosis. The described effects of RS 2518 on cancer cells have led to its selection as a lead compound for further studies. Some analogues have been developed and tested on a panel of cancer cell lines.

References

  1. Oncogene. 2003 Dec 8;22(56):9075-86 - PubMed
  2. Apoptosis. 2002 Aug;7(4):321-8 - PubMed
  3. J Med Chem. 2006 Feb 9;49(3):947-54 - PubMed
  4. Front Biosci. 2008 May 01;13:5138-54 - PubMed
  5. Expert Opin Investig Drugs. 2008 May;17(5):707-22 - PubMed
  6. Cancer Invest. 2005;23(3):264-73 - PubMed
  7. J Med Chem. 2009 Dec 10;52(23):7512-27 - PubMed
  8. J Med Chem. 2007 Jun 14;50(12):2865-74 - PubMed
  9. J Med Chem. 2004 Dec 2;47(25):6120-3 - PubMed
  10. Exp Cell Res. 2003 Oct 15;290(1):49-59 - PubMed
  11. Med Res Rev. 2007 Mar;27(2):209-38 - PubMed
  12. Int J Cancer. 2008 Jun 15;122(12):2674-81 - PubMed

Publication Types