scholarly journals Synthesis and Cytotoxicity of Chalcones and 5-Deoxyflavonoids

2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
Jing Zhang ◽  
Xin-Ling Fu ◽  
Nan Yang ◽  
Qiu-An Wang

Chalcones1~8and 5-deoxyflavonoids9~22were synthesized in good yields by aldol condensation, Algar-Flynn-Oyamada reaction, glycosidation, and deacetylation reaction, respectively, starting from 2-acetyl phenols substituted by methoxy or methoxymethoxy group and appropriately benzaldehydes substituted by methoxy, methoxymethoxy group, or chlorine. Among them,13and17~22are new compounds. The cytotoxicity bioassays of these chalcones and 5-deoxyflavonoids were screened using the sulforhodamine B (SRB) protein staining method, and the results showed that compounds2, 4, 5, 6, 10, 15, and19exhibited moderate cytotoxicity against the cancer cell line of MDA-MB-231, U251, BGC-823, and B16 in comparison with control drugs (HCPT, Vincristine, and Taxol).

2021 ◽  
Vol 14 (9) ◽  
pp. 853
Author(s):  
Islam Zaki ◽  
Sara A. Abu El-ata ◽  
Eman Fayad ◽  
Ola A. Abu Ali ◽  
Ali H. Abu Almaaty ◽  
...  

A new series of 2,4-disubstituted benzo[g]quinoxaline molecules have been synthesized, using naphthalene-2,3-diamine and 1,4-dibromonaphthalene-2,3-diamine as the key starting materials. The structures of the new compounds were confirmed by spectral data along with elemental microanalyses. The cytotoxic activity of all synthesized benzo[g]quinoxaline derivatives was assessed in vitro against the breast MCF-7 cancer cell line. The tested molecules revealed good cytotoxicity toward the breast MCF-7 cancer cell line, especially compound 3. The results of topoisomerase IIβ inhibition assay revealed that compound 3 exhibits potent inhibitory activity in submicromolar concentration. Additionally, compound 3 was found to cause pre-G1 apoptosis, and slightly increase the cell population at G1 and S phases of the cell cycle profile in MCF-7 cells. Finally, compound 3 induces apoptosis via Bax activation and downregulation of Bcl2, as revealed by ELISA assay.


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.


2001 ◽  
Vol 120 (5) ◽  
pp. A336-A336
Author(s):  
M SHIMADA ◽  
A ANDOH ◽  
Y ARAKI ◽  
Y FUJIYAMA ◽  
T BAMBA

2006 ◽  
Vol 175 (4S) ◽  
pp. 201-201 ◽  
Author(s):  
Isao Hara ◽  
Junya Furukawa ◽  
Kazuki Yamanaka ◽  
Yuji Yamada ◽  
Masato Fujisawa

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