Synthesis and biological evaluation of nitric oxide-releasing hybrids from gemcitabine and phenylsulfonyl furoxans as anti-tumor agents

MedChemComm ◽  
2015 ◽  
Vol 6 (6) ◽  
pp. 1130-1136 ◽  
Author(s):  
Xianghua Li ◽  
Xuemin Wang ◽  
Chenjun Xu ◽  
Junkai Huang ◽  
Chengniu Wang ◽  
...  

Novel furoxan/gemcitabine hybrids displayed significant antitumor activities, in particular 10e, which could be independent of the nucleoside transporter, release high levels of NO, and induce cell apoptosis by regulating apoptotic related proteins in tumor cells in vitro.

2013 ◽  
Vol 78 (9) ◽  
pp. 1301-1308 ◽  
Author(s):  
Lin Luo ◽  
Jiang-Ke Qin ◽  
Zhi-Kai Dai ◽  
Shi-Hua Gao

Nine novel aminoalkoxy substituted benzoxanthones (3a-3i) were synthesized. Their antitumor activities were evaluated in five human solid tumor cell lines including Hep-G2, BEL-7402, HeLa, MGC-803 and CNE by MTT method. The results showed that most of the compounds displayed moderate to good inhibitory activities on the tested cancer cell lines in vitro, among them compounds 3a and 3h showed higher antitumor activity than other tested compounds against most cell lines. The influence of two kinds of structural factors including the terminal amino group and length of carbon spacers on the anticancer activities were explored to discuss the preliminary structure-activity relationships.


2016 ◽  
Vol 71 (3) ◽  
pp. 205-210 ◽  
Author(s):  
Ali Almasirad ◽  
Loghman Firoozpour ◽  
Maliheh Nejati ◽  
Najmeh Edraki ◽  
Omidreza Firuzi ◽  
...  

AbstractA series of novel 1,3,4-thiadiazole derivatives bearing an amide moiety were designed, synthesized, and evaluated for their in vitro antitumor activities against HL-60, SKOV-3 and MOLT-4 human tumor cell lines by MTT assay. Ethyl 2-((5-(4-methoxybenzamido)-1,3,4-thiadiazol-2-yl)thio)acetate (5f) showed the best inhibitory effect against SKOV-3 cells, with an IC50 value of 19.5 μm. In addition, the acridine orange/ethidium bromide staining assay in SKOV-3 cells suggested that the cytotoxic activity of 5f occurs via apoptosis.


2011 ◽  
Vol 8 (1) ◽  
pp. 76-81 ◽  
Author(s):  
Liang Ge ◽  
jingjie Wang ◽  
Xiaoyan Zhang ◽  
Huibin Zhang ◽  
Hai Qian ◽  
...  

2008 ◽  
Vol 19 (2) ◽  
pp. 149-152 ◽  
Author(s):  
Xiang Wen Kong ◽  
Yi Hua Zhang ◽  
Li Dai ◽  
Hui Ji ◽  
Yi Sheng Lai ◽  
...  

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