RT Journal Article
T1 Synthesis and antimalarial and anticancer evaluation of  7‐chlorquinoline‐4‐thiazoleacetic derivatives containing aryl  hydrazide moieties
A1 Ramírez, Hegira
A1 Fernández Moreira, Esteban
A1 Mayora, Soriuska
A1 Martínez, Gricelis
A1 De Sanctis, Juan B.
A1 Celis, Carmen
A1 Charris, Jaime
AB Twelve 7-chloroquinoline derivatives were designed and synthesized using the principle of molecular hybridization through the coupling of 2-[2-(7-chloroquinolin-4-ylthio)-4-methylthiazol-5-yl]acetic acid 1 with various benzoyl hydrazines 2a–l. The synthetic compounds were tested as antimalarials. Some of them showed an efficient in vitro activity as inhibitors of β-hematin formation and an in vivo activity in a murine model, resulting in compounds 8 and 9 as the most active ones with IC50 values of 0.65 ± 0.09 and 0.64 ± 0.16 µM, respectively. The effects of the compounds on the cell viability, cell cycle, and apoptosis induction of A549 and MCF-7 cancer cell lines were also examined. Our data showed that compounds 6 and 12 were the most active agents, decreasing the cell viability of MCF-7 cells with IC50 values of 15.41 and 12.99 µM, respectively. None of the compounds analyzed significantly affected the viability of peripheral blood mononuclear cells. Also, significant induction of apoptosis was observed when both cancer cell lines were incubated with compounds 6 and 12. In MCF-7 cells, treatment with these compounds led to cell cycle arrest in the G0/G1 phase. The results obtained suggest that these structures may be useful in developing new therapies for malaria and cancer treatment.
PB Wiley
SN 0365-6233
YR 2021
FD 2021-04-08
LK https://hdl.handle.net/20.500.14352/124997
UL https://hdl.handle.net/20.500.14352/124997
LA eng
NO H. Ramírez, E. Fernandez, J. Rodrigues, S. Mayora, G. Martínez, C. Celis, J. B. De Sanctis, M. Mijares, J. Charris, Arch. Pharm. 2021, e2100002.
NO Instituto de Investigaciones Farmacéuticas
NO Universidad Central de Venezuela
DS Docta Complutense
RD 31 dic 2025