Objective: Cancer has become the major disease by uncontrolled cell growth effecting large population on the globe. This study, deals with antiproliferative activity of different solvent extracts, viz., n-hexane (S 1 ), dichloromethane (DCM) (S 2 ), and methanol (S 3 ) of Acacia farnesiana pod on four cancer cell lines, viz., chronic myelogenous leukemia (K562), breast cancer (MCF-7), hepatocellular carcinoma (HePG2), colorectal adenocarcinoma (Colo 205), and DNA cleavage activity of the extracts on CT-DNA. Methods:The antiproliferative study was performed by MTT assay and DNA cleavage studies of the solvent extracts (S 1 , S 2 , and S 3 ) and its fractions (S 4 and S 5 ) was carried out by agarose gel electrophoresis method. Results:The antiproliferative activity results revealed that n-hexane extract (S 1 ) has showed activity against MCF-7 (21.70 %) cell line and methanol extract (S 3 ) against K562 (24.5%) and HePG2 (23.3%) cell lines. The DNA cleavage could be seen at every concentration tested by n-hexane (S 1 ), DCM (S 2 ), and methanol (S 3 ) extracts and significant cleavage was observed at concentrations of 25, 50, and 100 µg by fractions (S 4 ) and (S 5 ) of methanol extract. Conclusion:The results indicated that the extract of A. farnesiana pod (n-hexane and methanol) has antiproliferative properties and the DNA cleavage studies performed on CT-DNA was found that the extracts and its fractions showed significant activity at the concentrations tested.
A novel series of 2-(5-alkyl-1,3,4-oxadiazol-2-yl)-3H-benzo[f]chromen-3-ones (4a-e) have been evaluated for analgesic, antibacterial and antiviral activities. Analgesic activity was carried out using acetic acid-induced writhing method in Swiss albino male mice. The antibacterial activity was performed against Gram-positive and Gram-negative clinical strains by agar well diffusion method. The in vitro antiviral activity was carried out against camelpox and buffalopox viruses. The analgesic activity exhibited by the compounds 4a, 4c and 4d were found to be more significant compared to the standard. The bacterial activity was determined by the inhibition of growth of the organism by the drugs at different concentrations. All the compounds showed significant activity when compared with the drug ciprofloxacin. The in vitro antiviral activity of the compound 4b tested against camelpox and buffalopox viruses revealed no activity when tested at concentrations of 250 μg. The compound 4b did not alter the titres of both the viruses and the titres remain, respectively, 106.5 TCID50 and 106.74 TCID50 per ml for camelpox vaccine virus and buffalopox vaccine virus. However, the compounds 4a-e showed significant analgesic and antibacterial activities.
Objective: Synthesis and antiproliferative study of novel 4-(piperidin-1-ylmethyl)-2-(thiophen-2-yl) quinoline 7(a-j) derivatives.Methods: 4-(piperidin-1-ylmethyl)-2-(thiophen-2-yl) quinolines were synthesized by the addition of 4-(chloromethyl)-2-(thiophen-2-yl) quinoline (0.01 mol), piperidine (0.01 mol) in DMF (10 v) and K 2 CO 3 ( 0.02 mol). The anticancer activity of the title compounds performed against T-47D, HeLa, HepG2, and MCF-7 human cancer cell lines growth was investigated by MTT assay. Results:The compounds 7b and 7g exhibited 90% of the growth inhibitory effect on T-47D, HeLa, and MCF-7 and also 80% growth inhibition in HepG2 when compared with standard drug paclitaxel. Conclusion:The synthesized compounds 4-(piperidin-1-ylmethyl)-2-(thiophen-2-yl) quinoline 7(a-j) exhibited a considerable degree of growth inhibition of human cancer cell lines. The synthesized molecules 7(a-j) are in acceptable range and are less toxic and can be considered as possible hits for drug discovery.In continuation of search on new compounds for antiproliferation treatment from our laboratory [28][29][30][31][32], we discovered that 2-(1-benzofuron-2-yl) quinoline-4-carboxylic acid and its esters [28] and 2-(benzofuran-2-yl)-4-(5-phenyl-4H-1,2,4-triazol-3-yl) quinoline and its derivatives [29] have possessed appreciable cytotoxic properties. Hence, the present work deals with the synthesis and antiproliferative potential of 4-(piperidin-1-ylmethyl)-2-(thiophen-2-yl) quinoline and its derivatives, along with detailed in silico pharmacokinetic and druglikeness properties Scheme 1. METHODS MaterialsCommercially available chemicals are used in the synthesis of compounds 7(a-j). The compounds were purified by column chromatography using silica gel 100-200 mesh with occasional monitoring by pre-coated aluminum thin layer chromatography (TLC) plates procured from Merck. Melting points were recorded by the open capillary method and are uncorrected by Raga Melting Point Apparatus. The 1 H-nuclear magnetic resonance (NMR) and 13 C-NMR spectra were recorded on a 400 MHz and 100 MHz, Bruker spectrometer using CDCl 3 as solvent and TMS as an internal standard. Mass spectra were recorded on the liquid chromatography-mass spectrometry Agilent mass spectrometer. Method 2-(1-thiophene-2-yl)quinoline-4-carboxylic acid 3(a-b)Isatin 1(a-b) (0.01 mol) and ethanol (10 v) were taken in a round bottom flask, to this 33% aq. KOH was added dropwise at 0-5°C followed by addition of 2-acetylthiophene 2 (0.01 mol). The reaction was refluxed at 75°C for 8 h. After completion, the reaction mixture was neutralized with dilute HCl. The precipitate, thus, formed was filtered, washed with ethyl acetate to remove impurities and dried to get compound 3(a-b). Methyl 2-(1-thiophene-2-yl) quinolone-4-carboxylates 4(a-b)2-(1-thiophene-2-yl) quinoline-4-carboxylic acid 3(a-b) (0.01 mol) was taken in methanol (10 v) in a round bottom flask, to this two drops of Conc. H 2 SO 4 was added. The reaction was refluxed at 75°C for 8 h. After completion, the reaction mixt...
Objective: The objective of the study is acetylcholinesterase (AChE) inhibitory effect of 3-(1H-indol-3-yl)-1, 3-diphenylpropan-1-one derivatives by Ellman's method, physostigmine is used as positive control.Method: 3-(1H-indol-3-yl)-1, 3-diphenylpropan-1-one derivatives were synthesized by the addition of chalcone (0.25 g, 1 mmol), indole (0.12 g, 1 mmol) in ethanol (5 ml), and concentrated hydrochloric acid (5 mmol %). These earlier synthesized compounds were screened for AChE inhibitors by modifying Ellman's method.Results: Among the tested compounds, 3a and 3j were found to be having more potential than other compounds with half maximal inhibitory concentration values of 13.64 and 14.3 µg/ml, respectively. Whereas, compounds 3c, 3e, 3g, and 3i exhibited an average AChE inhibition of 16.4, 17.9, 17.6, and 21.1 µg/ml, respectively. Conclusion:The compounds 3-(1H-indol-3-yl)-1, 3-diphenylpropan-1-one derivatives were found to be possible lead molecules in AChE inhibition and even though, the molecules were structurally dissimilar to that of the standard, still they exhibited a considerable degree of inhibition and encourage the researchers to look into the mode of action of their inhibition ability against AChE.
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