| Autor: |
Butler-Fernández KM; Department of Pharmaceutical Sciences, University of Puerto Rico, School of Pharmacy, San Juan 00936, Puerto Rico., Ramos Z; Department of Pharmaceutical Sciences, University of Puerto Rico, School of Pharmacy, San Juan 00936, Puerto Rico., Francis-Malavé AM; Department of Biology, College of Natural Sciences, University of Puerto Rico, San Juan 00931, Puerto Rico., Bloom J; Department of Pharmaceutical Sciences, University of Puerto Rico, School of Pharmacy, San Juan 00936, Puerto Rico., Dharmawardhane S; Department of Biochemistry, University of Puerto Rico, School of Medicine, San Juan 00936, Puerto Rico., Hernández E; Department of Pharmaceutical Sciences, University of Puerto Rico, School of Pharmacy, San Juan 00936, Puerto Rico. eliud.hernandez@upr.edu. |
| Abstrakt: |
In this study, a new series of N -alkyl-3,6-dibromocarbazole and N -alkyl-5-bromoindole derivatives have been synthesized and evaluated in vitro as anti-cancer and anti-migration agents. Cytotoxic and anti-migratory effects of these compounds were evaluated in MCF-7 and MDA-MB-231 breast cancer cell lines and an insight on the structure-activity relationship was developed. Preliminary investigations of their anti-cancer activity demonstrated that several compounds have moderate antiproliferative effects on cancer cell lines with GI 50 values in the range of 4.7-32.2 µM. Moreover, carbazole derivatives 10 , 14 , 15 , 23 , and 24 inhibit migration activity of metastatic cell line MDA-MB-231 in the range of 18-20%. The effect of compounds 10 , 14 , and 15 in extension of invadopodia and filopodia was evaluated by fluorescence microscopy and results demonstrated a reduction in actin-based cell extensions by compounds 10 and 15 . |
