Arylthioindoles: Promising compounds against cancer cell proliferation

作者:Giansanti Vincenzo; Piscitelli Francesco; Camboni Tania; Prosperi Ennio; La Regina Giuseppe; Parks Michele; Silvestri Romano; Scovassi Anna Ivana*
来源:Oncology Letters, 2010, 1(1): 109-112.
DOI:10.3892/ol_000000020

摘要

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

  • 出版日期2010-2