We found a match
Your institution may have access to this item. Find your institution then sign in to continue.
- Title
Novel conformationally constrained pyrazole derivatives as potential anti-cancer agents.
- Authors
Kasiotis, Konstantinos M.; Tzanetou, Evangelia N.; Haroutounian, Serkos A.; Stagos, Dimitrios; Koutsotheodorou, Eleni; Kouretas, Dimitrios; Fokialakis, Nikolas
- Abstract
The synthesis of 17 novel conformationally constrained pyrazole derivatives is reported herein, along with the assessment of their anti-proliferative and anti-angiogenic activities. The evaluation of their inhibitory effect on cell proliferation against HepG2, HeLa, and MCF-7 cells revealed the pyrrolo[2,3-g]indazole 23 as a potent inhibitor of cell growth with IC50 values of 5 μm. Additionally, the inhibition of vascular endothelial growth factor by pyrazoles 20 and 23 (30 % and 35 %, respectively) in HeLa supernatant cells was evidenced. These findings highlight the usefulness of these compounds as potential scaffolds for the design and development of novel anti-cancer agents with pronounced anti-angiogenic activity.
- Subjects
NEOVASCULARIZATION; ANTINEOPLASTIC agents; PYRAZOLES; INHIBITORY postsynaptic potential; CELL proliferation
- Publication
Zeitschrift für Naturforschung B: A Journal of Chemical Sciences, 2015, Vol 70, Issue 9, p677
- ISSN
0932-0776
- Publication type
Article
- DOI
10.1515/znb-2015-0053