In vitro toxicity evaluation in the development of new anticancer drugs—genistein glycosides

Crateva adansonii DC, an African ethnomedicinal plant, exerts cytotoxicity in vitro and prevents experimental mammary tumorigenesis in vivo

“…Furthermore, C. adansonii extract displayed a selective index Z1.73 against the ER-positive breast cancer cell line which is of interest for the research of alternative breast cancer treatment (Ovadje et al, 2015). This suggests that tumour cells may be 0.73 fold more sensitive to active principle of C. adansonii than normal cells (Bézivin et al, 2003;Popiołkiewicz et al, 2005). As displayed in phytochemical analysis, C. adansonii extract contains flavonoids, which, can account for its cytotoxicity because flavonoids are described as cytotoxic in vitro (Hakimuddin et al, 2004;Mansoor et al, 2011).…”

Potent genistein derivatives as inhibitors of estrogen receptor alpha-positive breast cancer

“…The reaction mixture was diluted with Ethylacetate and water, and the organic layer separated was concentrated and recrystallized in Ethylacetate and hexane mixture to yield product 17 (0.025 g, 71.4%). (18). To the genistein 2 (0.2 g, 0.74 mmol) in acetone (20 mL) was added K 2 CO 3 (0.35 g, 2.5 mmol) followed by the addition of 0.99 g, 4.4 mmol of the bromide shown in scheme 5.…”

Genistein Derivatization – From a Dietary Supplement to a Pharmaceutical Agent

“…Our observations were recently confirmed by others (Ahmed et al, 2011). Earlier studies shown that the structure of G21 molecule was stable, it did not hydrolyze under in vitro cell culture conditions (Ksycińska et al, 2004) and its toxicity against cancer cells was higher than against normal ones (Popiołkiewicz et al, 2005). The continuation of our work on glyconjugates of genistein exhibiting antimitotic activity pointed another molecule, called Ram3 (Fig.…”