Novel conformationally constrained pyrazole derivatives as potential anti-cancer agents
AuthorKasiotis, K. M.; Tzanetou, E. N.; Stagos, D.; Fokialakis, N.; Koutsotheodorou, E.; Kouretas, D.; Haroutounian, S. A.
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 mu m. 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 anticancer agents with pronounced anti-angiogenic activity.