Journal
ARCHIV DER PHARMAZIE
Volume 354, Issue 7, Pages -Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ardp.202100002
Keywords
antimalarial; antiproliferative; apoptosis; hydrazides; quinoline; thiazol
Funding
- Instituto de Investigaciones Farmaceuticas (IIF)
- Consejo de Desarrollo Cientifico y Humanistico de la Universidad Central de Venezuela (CDCH-UCV) [IIF.01-2014, 09-8819-2013/2, S1N1 2017-USB]
Ask authors/readers for more resources
Twelve 7-chloroquinoline derivatives were synthesized using molecular hybridization, showing potential as antimalarials and anticancer agents. Compounds 8 and 9 were the most active, particularly against MCF-7 cells. These compounds may be promising for developing new therapies for malaria and cancer treatment.
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 beta-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 mu M, 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 mu M, 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.
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