Growth inhibition of breast cancer by two flexible heteroarotinoid enantiomers
Growth inhibition of breast cancer by two flexible heteroarotinoid enantiomers
Emily Ginn1, Jenny Beak1, Hongye Zou1, Maryam M.J. Fallatah1, Erica Cayton1, Shengquan Liu2, Maggie Louie1, 2.
1Department of Natural Science and Mathematics, Dominican University of California, San Rafael, CA 94901, USA
2College of Pharmacy, Touro University-California, Vallejo, CA 94592, USA
Abstract/Description
Flexible heteroarotinoid (Flex-Hets) are compounds that show promising anti-cancerous activities. SHetA2, a first-generation Flex-Het, has been shown to block the growth of cervical, head and neck, kidney, lung, ovarian, prostate, and breast cancers. A second generation of compounds was developed to improve SHetA2’s high lipophilicity, limited selectivity, low bioavailability, and its complicated synthesis. Results from our recent study suggest that one of these analogs, 1-(1-(naphthalen-1-yl)ethyl)-3-(4-nitrophenyl) thiourea (SL-1-09) exhibits anti-cancer activities against ERα+ and ERα- breast cancer cells at micromolar concentrations. SL-1-09 is a mixture of enantiomers, R (SL-1-29) and S (SL-1-30), which were synthesized and purified for further analysis. The goal of this project is to determine the anticancer activity of SL1-29 and SL-1-30.
Growth inhibition of breast cancer by two flexible heteroarotinoid enantiomers
Guzman 201
Flexible heteroarotinoid (Flex-Hets) are compounds that show promising anti-cancerous activities. SHetA2, a first-generation Flex-Het, has been shown to block the growth of cervical, head and neck, kidney, lung, ovarian, prostate, and breast cancers. A second generation of compounds was developed to improve SHetA2’s high lipophilicity, limited selectivity, low bioavailability, and its complicated synthesis. Results from our recent study suggest that one of these analogs, 1-(1-(naphthalen-1-yl)ethyl)-3-(4-nitrophenyl) thiourea (SL-1-09) exhibits anti-cancer activities against ERα+ and ERα- breast cancer cells at micromolar concentrations. SL-1-09 is a mixture of enantiomers, R (SL-1-29) and S (SL-1-30), which were synthesized and purified for further analysis. The goal of this project is to determine the anticancer activity of SL1-29 and SL-1-30.