scholarly journals Synthesis and Antiproliferative Activity of Some Quinoline and Oxadiazole Derivatives

2016 ◽  
Vol 2016 ◽  
pp. 1-10 ◽  
Author(s):  
Mohamed Jawed Ahsan ◽  
Sunil Shastri ◽  
Rita Yadav ◽  
Mohd. Zaheen Hassan ◽  
Mohammed Afroz Bakht ◽  
...  

In continuance of our search for newer antiproliferative agents we report herein the synthesis and antiproliferative studies of two series (5a–j and 10a–c) of heterocyclic compounds. All the new compounds were characterized by IR, NMR, and mass spectral data. The antiproliferative activity of 10 compounds (5a–j) was carried out on HeLa (cervix cancer cell line) and MDA-MB-435 (melanoma) and LC50, TGI, and GI50 were calculated, while the antiproliferative activity of 3 compounds (10a–c) was carried out against nine different panels of nearly 60 cell lines (NCI-60) according to the National Cancer Institute (NCI US) Protocol at 10 μM. 1-(7-Hydroxy-4-methyl-2-oxoquinolin-1(2H)-yl)-3-(4-methoxylphenyl)urea (5j) was found to have antiproliferative activity with GI50 of 35.1 μM against HeLa (cervix cancer cell line) and 60.4 μM against MDA-MB-435 (melanoma), respectively. The compounds 10a, 10b, and 10c showed antiproliferative activity with comparatively higher selectivity towards HOP-92 (Non-Small Cell Lung Cancer) with percent growth inhibitions (GIs) of 34.14, 35.29, and 31.59, respectively.

2010 ◽  
Vol 5 (5) ◽  
pp. 1934578X1000500 ◽  
Author(s):  
Ende Pan ◽  
Shugeng Cao ◽  
Peggy J. Brodie ◽  
James S. Miller ◽  
Rolland Rakotodrajaona ◽  
...  

Investigation of a Malagasy endemic plant identified as Symphonia pauciflora Baker (Clusiaceae) for antiproliferative activities against the A2780 ovarian cancer cell line led to the isolation of a new compound identified as 2-(3,3-dimethylallyl)-7-methoxy-1,5,6-trihydroxy-2″″,2″″-dimethylpyrano(6″″,5″″:3,4) xanthone (1) and the two known guttiferones A (2) and I (3). The structure elucidation of 1 was based on the analysis of its 1D and 2D NMR and mass spectral data. Compound 1 showed good antiproliferative activity with an IC50 value of 3.8 μM against the A2780 human ovarian cancer cell line, while the known guttiferone analogues (2 and 3) exhibited moderate activities with IC50 values of 8.3 μM and 7.8 μM, respectively.


ChemInform ◽  
2010 ◽  
Vol 41 (42) ◽  
Author(s):  
Yong-Miao Shen ◽  
Peng-Cheng Lv ◽  
Wu Chen ◽  
Peng-Gang Liu ◽  
Ming-Zhu Zhang ◽  
...  

2010 ◽  
Vol 45 (7) ◽  
pp. 3184-3190 ◽  
Author(s):  
Yong-Miao Shen ◽  
Peng-Cheng Lv ◽  
Wu Chen ◽  
Peng-Gang Liu ◽  
Ming-Zhu Zhang ◽  
...  

2014 ◽  
Vol 893 ◽  
pp. 512-515 ◽  
Author(s):  
Lu Jiang ◽  
Bin Zeng

Based on the study of rhodanine derivative WL-276,some novel compounds were synthesized,and their anti-tumor effects were screened by MTT method. Hydantoin is rhodanine of electronic derivative. Compounds of 3a-3d were obtained by Aldol reaction, whose structures were confirmed by 1H-NMR. Furthermore, preliminary pharmacological results suggested that compounds 2a had strong inhibitory effects on the proliferation of HepG2 tumor cells.


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