Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 132, Issue -, Pages 63-80Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2017.03.028
Keywords
Isothiocyanates; Isothiocyanatoalkylphosphonates; IC50; Apoptosis; Cell cycle arrest; 4T1 murine mammary gland cancer; Tumor growth inhibition
Categories
Funding
- Polish National Science Centre [DEC 2011/03/B/ST5/01058, DEC 2011/01/N/NZ4/03361]
- Wroclaw University of Technology [S30134/Z0313]
- Wroclaw Center of Biotechnology within the Leading National Research Center (KNOW) program
Ask authors/readers for more resources
A library of over forty, novel, structurally diverse phosphonate analogs of sulforaphane (P-ITCs) were designed, synthesized and fully characterized. All compounds were evaluated for antiproliferative activity in vitro on Lovo and LoVo/DX colon cancer cell lines. All compounds exhibited high antiproliferative activity, comparable or higher to the activity of naturally occurring benzyl isothiocyanate and sulforaphane. Assessment of the mechanisms of action of selected compounds revealed their potential as inducers of G(2)/M cell cycle arrest and apoptosis. Further antiproliferative studies for selected compounds with the use of a set of selected cell lines derived from colon, lung, mammary gland and uterus as well as normal murine fibroblasts were performed. In vivo studies of the analyzed phosphonate analogs of sulforaphane showed lower activity in comparison with those of benzyl isothiocyanate. Our studies demonstrated that newly synthesized P-ITCs can be used for as a starting point for the synthesis of novel isothiocyanates with higher anticancer activity in the future. (C) 2017 Elsevier Masson SAS. All rights reserved.
Authors
I am an author on this paper
Click your name to claim this paper and add it to your profile.
Reviews
Recommended
No Data Available