A novel series of potent cytotoxic agents targeting G2/M phase of the cell cycle and demonstrating cell killing by apoptosis in human breast cancer cells.
Breast cancer, a leading cause of mortality in women, warrants the development and biological evaluation of new anticancer agents. A novel series of thiopyridine triazine derivatives was synthesized and investigated in the human breast cancer cell line, MDA-MB-468. SM40, the most potent derivative, induced a G2/M arrest and apoptosis with a possible involvement of p53. The cytotoxicity of SM40 was also examined against the NCI 60 cell line panel and its potency was rationalized using molecular modeling. Results suggest that SM40 is a promising cytotoxic agent.
Mandal
Soma
S
Faculty of Medicine, Memorial University of Newfoundland, St John's, NL, Canada.
Bérubé
Gervais
G
Asselin
Eric
E
Mohammad
Iqbal
I
Richardson
Vernon J
VJ
Gupta
Atul
A
Pramanik
Saroj K
SK
Williams
Arthur L
AL
Mandal
Sanat K
SK
D000970:Antineoplastic Agents / Q000494:pharmacology*; D017209:Apoptosis; D001943:Breast Neoplasms / Q000188:drug therapy*; D002455:Cell Division; D045744:Cell Line, Tumor; D015195:Drug Design; D004354:Drug Screening Assays, Antitumor; D016195:G2 Phase; D006801:Humans; D006860:Hydrogen Bonding; D008956:Models, Chemical; D008958:Models, Molecular; D008968:Molecular Conformation; D011725:Pyridines / Q000737:chemistry; D014227:Triazines / Q000737:chemistry
D000970:Antineoplastic Agents; D011725:Pyridines; D014227:Triazines