Current Issue : April - June Volume : 2014 Issue Number : 2 Articles : 6 Articles
In the present investigation, a series of novel N-substituted 5-arylidenerhodanine was designed and further synthesized from their corresponding aromatic aldehydes according to Knoevenagel�s condensation method in microwave conditions. The resulting 5-arylidinerhodanine was reacted with 2-phenylethyl chloride in presence of potassium carbonate and dimethyl formamide under microwave conditions to give N-substituted 5-arylidenerhodanine. The synthesized compounds were confirmed on the basis of spectral data and elemental analyses. The synthesized compounds evaluated for their cytotoxic activity against two different human cancer cell lines using MTT assay. The cytotoxic activity results revealed that the synthesized compounds demonstrated the ability to inhibit HT-29 (colon cancer), MCF-7 (breast cancer) cancer cell lines against reference drug Methotrexate. Among the compounds tested, the most active compounds (4-trifluoro and 3-fluoro-substituted) possess significant cytotoxic activity against both the cancer cell lines and all other compounds showed moderate to weak activity....
N-phenylacridin-9-amine derivative having anticancer activity on the human nasopharyngeal carcinoma (HONE-1)\r\ncell line, human adenocarcinoma (colon and rectal) tumor (HT-29) cell line, human brain tumor (DBTRG) cell line, gastric\r\ncarcinoma TSGH, hepatoma liver Hepa-G2, mouth carcinoma KB, lung adenocarcinoma H460, breast adenocarcinoma MX-1 and\r\nMCF-7 cell line and it�s significant cytotoxic activity against human leukemic HL-60 cell growth. N-phenylacridin-9-amine\r\nderivative exhibit both in-vivo as well as in-vitro potent antitumor activity. The alkylcarbamates of the N-phenylacridin-9-amine\r\nis more effective than their corresponding parent N-phenylacridin-9-amine derivatives. The cytotoxic activity of the Nphenylacridin-\r\n9-amine ethylcarbamates is decreased with increasing length and size of the alkyl function. It is also having drug-\r\nDNA binding affinity which affects the antitumor activity of 9-anilinoacridines. These compound having higher cytotoxic activity\r\ndue to high lipophilicity. We have used 25 compounds and those pIC50 activities on the HONE-1 cell line for the 2-D QSAR study.\r\nHere the 2D-QSAR studies of N-phenylacridin-9-amine analogues were performed by using software chem-draw ultra-8.0,\r\nopenbable-2.2.1, dragon, valstat. We are considering here two model equations for QSAR study. The value of linearity r2 for\r\nmodel-1 of HONE-1 cell line (model-1) is; r2 = 0.88699, Q2 = 0.800012, Spress = 0.3513 and SDEP = 0.321972 while this value for\r\nmodel-2 of HONE-1 cell line is; r2 = 0.879216, Q2 = 0.784529, Spress = 0.364646 and SDEP = 0.334203. Both models were\r\nvalidated by the Valstat software....
Heterocyclic compounds being highly reactive found to possess various pharmacological activities. Among the various heterocyclic rings pyrimidines and pyrazolines play a vital role in biological processes as found in natural and also synthetic lead molecules. In the present study new pyrimidines and pyrazolines were synthesized via a,�Ÿ-unsaturated carbonyl compounds (Chalcones). The synthesized compounds were characterized by means of their IR, 1H NMR and Mass spectral data. The compounds were evaluated for anticonvulsant activity by maximal electro shock method and the compounds were proven to possess significant activity. The synthesized compounds were studied for druglikeliness by calculating druglikeliness descriptors. A theoretical approach is also made to these synthesized molecules to predict adverse effects using OSIRIS software which helps to develop lead molecules....
Thiazolidinone, a saturated form of thiazole with carbonyl group on fourth carbon, has been considered as a magic moiety (wonder nucleus) which posses almost all types of biological activities. This diversity in the biological response profile has attracted the attention to explore this skeleton to its multiple potential against several activities. Present article is sincere attempt to suggest chemistry, synthesis spectral studies and applications of 4-thiazolidinone, further docking studies were performed on synthesized novel compounds by using AutoDock 4.0 MGL tools software packages. This molecular modeling study allowed confirming the preferential binding mode of novel 4-thiazolidinones inside the active site....
Objective: Colorectal cancer (CRC) is the third most frequently occurring cancer in both male and females, but it ranks second in developed countries. The incidence of colorectal cancer is still increasing in large parts of the world due to the development of resistance to the available drugs. Thus, there is a need to develop novel colorectal anti cancer agents. Materials and Methods: The present work includes the synthesis of a series of new 7-(Substituted benzylidene)-3-aryl-2,3,4,5,6,7-hexahydroindazol-1-yl(pyridine-4-yl)methanones from substituted chalcones. These chalcones were prepared by Claisen-Schmidt reaction by the condensation of cyclohexanone and various substituted aromatic aldehydes. The synthesized compounds were confirmed by IR, 1H NMR, MASS spectra and CHNO Elemental analysis. The synthesized compounds were predicted for biological activities by Insilico method based on those predictions the compounds screened for colorectal anti cancer activity (MTT assay) by using cell line HT-29 human colorectal adenocarcinoma using cisplatin as standard drug. Results: The compounds 2a, 2c, 2f, 3a, 3c and 3f exhibited maximum activity at a concentration <10 �µg, 2b, 2e, 3b and 3e exhibited moderate activity at a concentration <20 �µg. Remaining compounds 2d and 3d exhibited no activity at concentration >30 �µg. Conclusion: The synthesized compounds having the electron releasing groups such as hydroxyl and dimethyl amino group in phenyl ring exhibited maximum activity. Hence it clearly indicates the importance of electron releasing groups on aromatic rings for anticancer activity....
Zolpidem based compounds affects GABAA regulation in locomotor activity and sleep. Aim: The study was undertaken to evaluate the effect of Zolpidem based derivatives in mice. Synthesis, Characterizations, biological profiling and molecular docking studies were carried out to understand the biological activity and binding selectivity of the synthesized compounds. Methods: The study indicates that substituted Zolpidem based compounds were shown potent phenobarbitone induced hypnosis as well as locomotor activity throughout the study. Molecular docking study by AutoDock 4.2 MGL tools helped to understand the hypothetical selectivity of the compounds and also endowed the future prospects of de novo design for future prototype ligands. Observation: Compound 7a and 7d produced significant reduction in onset and prolongation of sleep duration induced by phenobarbitone. In the second model(Locomotor activity in actophotometer) activity was found to be maximum for 7a and 7d (30 mg/kg), produced 31.2 and 33.2 % decreased in locomotors activity, where standard drug Phenobarbitone produced 59.37% decreased in activity. Molecular docking studies also concluded the selectivity of compound 7d was appreciable in respect to the standard. The binding energy and the bond distances of phenobarbitone and Compound 7d between the target were found to be -7.24 kcal, and -6.6 kcal and 2.829 Ã?â?¦ (PRO 85), 1.896 Ã?â?¦ (PHE 78), (LEU 76) respectively. Conclusion: The study revealed the possibilities in future research of Zolpidem based derivatives for establishment of new generation CNS acting agents....
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