A quinoline-2-thione derivative as a novel chemotherapy drug candidate displays anti-tumor activity in vitro and in vivo DOI Creative Commons
Jinjin Zhao, Jie Zhao, Fei Lin

et al.

BMC Cancer, Journal Year: 2024, Volume and Issue: 24(1)

Published: Oct. 13, 2024

Ovarian cancer is the fifth most prevalent in women. Chemotherapy a major treatment option for patients with advanced ovarian (OC). Quinoline-2-thione and its derivatives are potential candidates tumor therapy. In this study, we investigated anticancer activity of quinoline-2-thione derivative KA3D against cancer. The effect on viability cells was evaluated using MTT assay, effects apoptosis cell cycle were detected flow cytometry. Western blotting performed to identify apoptosis-and cycle-related proteins altered by treatment. A xenograft model used verify inhibitory vivo. H&E staining, biochemical indicator detection, blood counts observe toxicity side KA3D. impeded viability, induced apoptosis, G2 phase cells. Mechanistically, found that enhanced expression proapoptotic molecules such as BAX Caspase 3, while antiapoptotic BCL2 inhibited. G0/G1 phase-related protein cyclin D1 reduced B1 upregulated. vivo, displayed potent activity, no apparent BABLC/c nude mice bearing SKOV3 demonstrated remarkable chemotherapeutic drug efficacy terms significant suppression vitro vivo low toxicity.

Language: Английский

Advances in the Potential of Quinoline‐Derived Metal Complexes as Antimalarial Agents: A Review DOI Open Access
Carla Peron, Raoni S. B. Gonçalves, Sidnei Moura

et al.

Applied Organometallic Chemistry, Journal Year: 2025, Volume and Issue: 39(3)

Published: Feb. 11, 2025

ABSTRACT Quinolines obtained from native trees of South and Central America, the genus Cinchona , have been used since 17th century for treatment malaria. However, it was only in 1820 that quinine had its structure elucidated, subsequently, during 20th century, several synthetic derivatives were produced with superior activities. In parallel, search synthesis metal complex compounds malaria dates 1994, development ferroquine, an iron derived chloroquine, developed by Biot collaborators at Lille University. After, there are complexes synthesized various metals, such as ruthenium, gold, iridium, platinum, over last 30 years, which aims this review. This review identified 84 quinoline–metal reported across 25 studies, gold (Complex 63) showing significant potency against FcBI strain (IC 50 10 nM), outperforming chloroquine (CQ, indicating coordination enhances drug's action. The ruthenium 03) exhibited activity PFB but less effective than CQ 22.5 vs. 8.2 nM). Other complexes, Au(III) 61), Ir(I) 52), Ir(II) 50), also demonstrated promising results varying effectiveness different strains. Structural features, including linear geometry Au(I) square planar or piano stool geometries Ru(II) Ir play crucial roles influencing their biological activity. These findings highlight potential improving antimalarial efficacy.

Language: Английский

Citations

0
Quinoline schiff bases (QSBs) and their derivatives: emerging trends in antimicrobial agents DOI
Mansi Gandhi, Vishwajit Chavda,

Shashi V. Ranga

et al.

Journal of Coordination Chemistry, Journal Year: 2025, Volume and Issue: unknown, P. 1 - 34

Published: May 20, 2025

Language: Английский

Citations

0
The current landscape of 1,2,3‐triazole‐(fused) six‐membered nitrogen‐containing heteroaromatic ring hybrids with anticancer therapeutic potential DOI Open Access

Zhi Xu,

Rongqiang Li,

Zhiwei Huang

et al.

Archiv der Pharmazie, Journal Year: 2024, Volume and Issue: 358(1)

Published: Dec. 30, 2024

Cancer, characterized by uncontrolled growth and spread of abnormal cells potentially influencing almost all tissues in the body, is one most devastating lethal diseases throughout world. Chemotherapy principal approaches for cancer treatment, but multidrug resistance severe side effects represent main barriers to success therapy, creating a vital need develop novel chemotherapeutic agents. The 1,2,3-triazole moiety can be conveniently constructed "click chemistry" could exert diverse noncovalent interactions with various enzymes cells. Hence, fascinating anticancer pharmacophores. Moreover, also serve as powerful ligation tool complex molecular architectures increase efficacy lead molecules. Notably, 1,2,3-triazole-containing hybrids intriguing structural variations target different biological components simultaneously, highlighting their potential treatment eradication cancer. This review outlines current landscape 1,2,3-triazole-(fused) six-membered nitrogen-containing heteroaromatic ring hybrids, inclusive 1,2,3-triazole-quinazolines, 1,2,3-triazole-quinazolinones, 1,2,3-triazole-quinolines, 1,2,3-triazole-quinolones, 1,2,3-triazole-pyridines, 1,2,3-triazole-pyrimidines, therapeutic potential, explores mechanisms action, critical aspects design well structure-activity relationships (SARs), covering articles published from 2021 present, pave way development innovative efficient interventions therapy.

Language: Английский

Citations

2
A quinoline-2-thione derivative as a novel chemotherapy drug candidate displays anti-tumor activity in vitro and in vivo DOI Creative Commons
Jinjin Zhao, Jie Zhao, Fei Lin

et al.

BMC Cancer, Journal Year: 2024, Volume and Issue: 24(1)

Published: Oct. 13, 2024

Ovarian cancer is the fifth most prevalent in women. Chemotherapy a major treatment option for patients with advanced ovarian (OC). Quinoline-2-thione and its derivatives are potential candidates tumor therapy. In this study, we investigated anticancer activity of quinoline-2-thione derivative KA3D against cancer. The effect on viability cells was evaluated using MTT assay, effects apoptosis cell cycle were detected flow cytometry. Western blotting performed to identify apoptosis-and cycle-related proteins altered by treatment. A xenograft model used verify inhibitory vivo. H&E staining, biochemical indicator detection, blood counts observe toxicity side KA3D. impeded viability, induced apoptosis, G2 phase cells. Mechanistically, found that enhanced expression proapoptotic molecules such as BAX Caspase 3, while antiapoptotic BCL2 inhibited. G0/G1 phase-related protein cyclin D1 reduced B1 upregulated. vivo, displayed potent activity, no apparent BABLC/c nude mice bearing SKOV3 demonstrated remarkable chemotherapeutic drug efficacy terms significant suppression vitro vivo low toxicity.

Language: Английский

Citations

0