European Journal of Molecular & Clinical Medicine

Imidazole nucleus has been potential studied member from heterocyclic compound family. Imidazole and its derivatives showing good pharmacological activities against various diseases. Imidazole is the heterocyclic molecule which having   the  interesting physical and chemical properties, in the present article focus lies on analysis of these properties which in turn may be exploited for different pharmacological activities, like compounds having a 3,4,5-trimethoxyphenyl ring linked to either N-1 or C-4 position of the imidazole entity gave an interesting profile of cytotoxicity with specific activity against leukemia cell lines, combination of indole-imidazole compounds formed demonstrated substantial in vitro anti proliferative activities against cancer cell lines, effective substitutions are also made in the entity which resembles structures of various natural compounds whose anti cancerous activity has already been examined. The present review study highlighting pharmacological potential of the imidazole. In present study we have discussed compounds synthesized with imidazole moieties as their structural framework. Thus can say imidazole is a moiety which had been exploited in the past years for synthesizing various compounds having versatile pharmacological activities, and still it can be further utilized for future prospective against various pathological conditions and other uses

The antioxidant and anticancer activity dry fruit extract of ficus carica linn investigated against free radical scavenging activity (RSA) [reactions with 1,1-diphenyl-2-picrylhydrazyl radical (DPPH) and anticancer activity against Dalton’s ascitic lymphoma cell line and assessment of the influence of extracts on the enzyme xanthine oxidase (XO), and Fe3+ reducing ability. Antitumor activity was studied on swiss albino mice at various dose such as 250, 500, and 1000 mg/kg, body weight. The experimental parameter used were tumor volume, tumor cell count, viable tumor cell count, mean survival time and increase in life span to assess antitumor activity. The extract was administered orally for 14 consecutive days to tumor bearing group of animals. It increases the life span of DAL treated mice and restores the hematological parameters as compared with the DAL bearing mice in dose dependent manner. The study revealed that the extract of ficus carica (EFC) showed significant antitumor activity in tested animal models. 

A novel series of triazolylquinazolin-4-one derivatives have been synthesized and characterized by TLC, melting point, FT-IR, 1H NMR and mass spectroscopy data. The synthesized series of title compounds were subjected for docking studies using Schrodinger Glide software, evaluated for their potential to inhibit enzyme EGFR-tyrosine kinase followed by in-vitro anticancer activity by SRB assay method on HeLa, MCF-7, A-549 cell lines. The series of compounds shows anticancer activity probably by inhibiting the enzyme EGFR-tyrosine kinase.

The chemical structure of the newly synthesized compound Ethyl-6-methyl-2-oxo-4-(3,4,5-trichlorophenyl)-1,2,3,4-tetrahydropyrimidine-5-carboxylate 4 was confirmed by elemental analysis, 1H NMR, 13C NMR, and ESI-HRMS spectral data. In addition, in the form of the complete and partial density of states, the HOMO-LUMO energy gap, and electrostatic potential map, etc., some quantum chemical insights have been obtained. Furthermore, to demonstrate the possible applications of dihydropyrimidinone 4 in nonlinear optics, the polarizability and first hyperpolarizability were measured. Molecular docking is also determined in order to illustrate the over expression of estrogen receptor in 92 % of 2J9M protein. The antitumor activity of these compound was evaluated on breast cancer (MCF-7) cell lines by a cell viability assay utilizing the tetrazolium dye 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT). Although with varying degrees, a significant growth inhibitory and cytotoxic effect was observed on MCF-7 cancer cell line. The tested compound 4, was active against MCF-7 cell line (in-vitro analysis) with IC50 values of 45 μM. The compound was subjected for the DPPH & ABTS tests, evaluated its antioxidant activity. With further characterization, mechanism of biological action, this compound 4 shall be a potential / useful candidate as anticancer drug.