Abstract
AbstractSynthesis, anti-proliferative, DNA cleavage, and in silico ADMET studies of 2-(1-benzofuran-2-yl) quinoline-4-carboxylic acids and their resultant esters in acid catalyzed medium have been investigated. The synthesized compounds are characterized by UV, IR, 1H NMR, 13C NMR, and mass spectral analysis. The electrophoretic DNA cleavage studies on λ-DNA (Eco-RI/Hinda-III double digest) using agarose gel method and the antiproliferative activity was carried out by MTT assay on five different human cancer cell lines (Chronic Myelogenous Leukemia (K562), Breast Cancer (MCF-7), Cervical Cancer (HeLa), Colorectal Adino carcinoma (Colo 205), and Hepato cellular carcinoma (HepG2)). Doxorubicin is taken as standard for comparison. The cleavage study indicated that molecules (3b–6a and 7b–8c) did cleave the DNA completely with no trace of fragments. The molecules (6b, 6c and 7a) have appeared to cleave DNA partially and assessed by comparing the bands appeared in control and test compounds at 100 μg concentra...
Highlights
The mortality of patients suffering from various types of cancer has become an important issue worldwide
The results showed that of all the different derivatives, fluoro-substituted carboxylate has reasonable inhibition on different cancer cell lines
The cinchophen analogs are known for their varied medicinal properties and reported for various biological activities
Summary
The mortality of patients suffering from various types of cancer has become an important issue worldwide. The quinoline core system is an important structural fragment of a large number of synthetic compounds displaying biological activities such as antibacterial, antimalarial, antihypertensive, anti-asthmatic, and as anti-inflammatory (Bilker et al, 1998; Chen, Fang, Sheu, Hsu, & Tzeng, 2001; Larsen et al, 1996). Quinoline carboxylic acid and their analogs confirm wide assortment of medicinal properties including antitumor (Feng, DingQiao, Kai-Ling, & Wei, 2006), antiviral (Granik et al, 1978) and antibacterial activities (Nazrullaev, Bessonova, & Akhmedkhodzhaeva, 2001). The quinoline carboxylic acid and their analogs that could imitate ellipticene, exhibit considerable antitumor activity due to its DNA intercalating properties (Knölker & Reddy, 2002). It has been shown that quinolines reveal antitumor activity due to the enlargement of stable complex with DNA (Aravinda, Bhojya Naik, & Prakash Naik, 2010)
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