NDLI: Synthesis and antitumor activity of a new 7-azaindole derivative

Content Provider	Springer Nature Link
Author	Sui, Dayun Zhang, Peng Wang, Yingshi Sun, Weilun Wu, Yi Xu, Huali Yu, Xiaofeng Qu, Shaochun Hu, Jianbing
Copyright Year	2014
Abstract	We designed and synthesized a 7-azaindole derivative(TH1082), which was characterized by $^{1}$H NMR and $^{13}$C-NMR. We investigated its antitumor effects on human melanoma A375 cells, human liver cancer SMMC cells and human breast cancer MCF-7 cells in vitro via 3-(4,5-dimethyldiazol-2-yl)-2,5-diphenyl-tetrazolium bromide (MTT) assay and also explored the mechanism of antiproliferation of them. The results show that TH1082 significantly inhibited the proliferation of these cells to different extent. The IC$_{50}$ values for A375 cells, SMMC cells and MCF-7 cells were 25.38, 48.70 and 76.94 μg/mL at 24 h, respectively. To observe cell morphological changes, acridine orange/ethidium bromide(AO/EB) staining and Hoechest33342/PI staining were carried out. These results indicate that TH1082 could induced the apoptosis of A375 cells. The apoptotic rates were (9.5±2.09)%, (18.9±2.25)% and (39.5±2.02)%(5, 10 and 20 μg/mL) for A375, SMMC and MCF-7 cell lines, respectively. Further, we determined the activities of caspase-3 and caspase-9 in A375 cells treated with TH1082 at different concentrations(0, 5, 10 and 20 μg/mL) or Z-VAD-FMK(20 μmol/L), a pan-caspase inhibitor for 24 h. The results show that TH1082 activated caspase-3 and caspase-9, and the activation could be blocked by Z-VAD-FMK. Taken together, these findings indicate that TH1082 could inhibit the proliferation of A375 cells via activating caspase-3 and caspase-9.
Starting Page	420
Ending Page	424
Page Count	5
File Format	PDF
ISSN	10059040
Journal	Chemical Research in Chinese Universities
Volume Number	30
Issue Number	3
e-ISSN	22103171
Language	English
Publisher	Jilin University and The Editorial Department of Chemical Research in Chinese Universities
Publisher Date	2014-03-28
Publisher Place	Heidelberg
Access Restriction	One Nation One Subscription (ONOS)
Subject Keyword	Chemistry/Food Science Analytical Chemistry Physical Chemistry Antitumor 7-Azaindole Inorganic Chemistry Apoptosis Organic Chemistry
Content Type	Text
Resource Type	Article
Subject	Chemistry Education

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