Synthesis, Anti-Cancer and Anti-Migratory Evaluation of 3,6-Dibromocarbazole and 5-Bromoindole Derivatives

Molecules

Suranganie Dharmawardhane¹  AdelaM. Francis-Malavé²  KrystalM. Butler-Fernández³  Zulma Ramos³  Joseph Bloom³  Eliud Hernández³ 

[1] Department of Biochemistry, University of Puerto Rico, School of Medicine, San Juan 00936, Puerto Rico;Department of Biology, College of Natural Sciences, University of Puerto Rico, San Juan 00931, Puerto Rico;Department of Pharmaceutical Sciences, University of Puerto Rico, School of Pharmacy, San Juan 00936, Puerto Rico;

关键词: 3,6-dibromocarbazole;    5-bromoindole;    carbazole;    actin;    breast cancer;    migration;   

DOI  :  10.3390/molecules24152686

来源: DOAJ

【 摘 要 】

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 GI₅₀ 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.

【 授权许可】

Unknown