薬学および生命科学における研究開発の国際ジャーナル

抽象的な

CYTOTOXIC SYMMETRICAL THIAZOLEDISELENIDES WITH INCREASED SELECTIVITY AGAINST MCF-7 BREAST CANCER CELLS

Saad Shaaban, Hatem E. Gaffer, Mohannad Alshahd, and Saad S. Elmorsy

A novel series of symmetrical thiazolediselenides were synthesized in good to moderate yields and there in vitro cytotoxic activity was evaluated against
breast adenocarcinom (MCF-7) and compared with their cytotoxicity in normal fibroblast cells (WI-38) employing standard MTT assay. Additionally, there in vitro
antimicrobial activities were also evaluated against gram-negative (Escherichia coli), gram-positive (Staphylococcus aureus) bacteria and a pathogenic yeast
(Candida albicans). A significant difference in toxicity zones between breast solid tumor cells and normal WI-38 cells was observed indicating that it is not general
selenium toxicity. Within this context, compounds 4b, 5, 7, 18 and 23 exhibited therapeutic indices (TI) up to eleven fold and in most cases were higher than TI of 5-
fu suggesting their effectiveness as anti-cancer agents. On the other hand, compounds 4a, 5, 7, 18 and 22 exhibited good antibacterial activity against E. coli and
S. aureus bacteria compared to the known drug, ampicillin. Moreover, compounds 4a, 7, 11, 13, 19, 22 and 23 exhibited good antifungal activity against C.
albicans compared to colitrimazole. These initial promising results point to a reasonable activity of some of these compounds, which needs to be further investigated
by using a considerably wider arsenal of human cancer and normal cells as well as humanopathogenic bacteria and fungi.