Antiproliferative effects of a series of novel synthetic sulfonate esters on human breast cancer cell line MCF-7.
BACKGROUND
It has been well documented that some organosulfur compounds (OACs) show promise as anticancer agents.


METHODS
The growth inhibitory effects of six novel different synthetic sulfonate esters was evaluated on cancerous (MCF-7) and non-cancerous (MCF-10A) human breast epithelial cells.


RESULTS
We found that the most active compounds against MCF-7 breast cancer cells had a common structure of p-methoxyphenyl p-toluenesulfonate with the methoxy substituent shifted from position 4 (22) to 2 (22o) or to 3 (22m). 3-Methoxyphenyl p-toluenesulfonate (22m) showed the lowest IC50 value (89.83 microM) on breast cancer cells but was also very active on non-cancerous MCF-10A cells (IC50 value of 53.96 microM). We found that compound 22 caused a greater degree of cell cycle arrest and induced apoptosis in cancerous MCF-7 cells compared with normal breast epithelial MCF-10A cells. However, compound 22m, was less selective by significantly arresting normal cells at G2/M-phase followed by a weak induction of apoptosis.


CONCLUSIONS
P-methoxyphenyl p-toluenesulfonate (22) appeared to be a more selective inhibitor of the growth of human breast cancer cells. Taken together, these results show that synthetic OSC compounds evaluated in this study can be effective antineoplastic agents and are worthy of further investigation.
Cyr
Louis
L
Laboratoire de biologie cellulaire et de thérapie génique, Département de biologie, Moncton, Université de Moncton, Moncton, New Brunswick E1A 3E9, Canada.
Langler
Richard F
RF
Crandall
Ian
I
Lavigne
Carole
C
D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D017209:Apoptosis; D001557:Benzenesulfonates / Q000737:chemistry / Q000494:pharmacology*; D001943:Breast Neoplasms; D002453:Cell Cycle / Q000187:drug effects; D002460:Cell Line; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D004952:Esters / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D013451:Sulfonic Acids / Q000737:chemistry / Q000494:pharmacology*
D000970:Antineoplastic Agents; D001557:Benzenesulfonates; D004952:Esters; C521355:P-methoxyphenyl p-toluenesulfonate; D013451:Sulfonic Acids