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 (RS2518) 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 G2/M cell cycle phase and inhibits cell proliferation, thus leading to apoptosis. The described effects of RS2518 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.
Arylthioindoles: Promising compounds against cancer cell proliferation / Giansanti, V.; Piscitelli, Francesco; Camboni, T.; Prosperi, E.; LA REGINA, Giuseppe; Parks, M.; Silvestri, Romano; Scovassi, A. I.. - In: ONCOLOGY LETTERS. - ISSN 1792-1074. - 1:(2010), pp. 109-112. [10.3892/ol_00000020]
Arylthioindoles: Promising compounds against cancer cell proliferation.
PISCITELLI, FRANCESCO;LA REGINA, GIUSEPPE;SILVESTRI, Romano;
2010
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 (RS2518) 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 G2/M cell cycle phase and inhibits cell proliferation, thus leading to apoptosis. The described effects of RS2518 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.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
