Anticancer activity of the synthetic kusunokinin analogues on human cancer cell lines
1
item.page.dc.date.issued
2025-01-15
item.page.dc.type
item.page.dc.identifier.issn
00404020
item.page.dc.identifier.eissn
14645416
item.page.dc.identifier.doi
item.page.dc.identifier.scopus
2-s2.0-85209404514
item.page.oaire.citation.title
Tetrahedron
item.page.oaire.citation.volume
170
item.page.dc.rights.holder
SCOPUS
item.page.dc.identifier.citation
Tetrahedron Vol.170 (2025)
punsarn.item.page.citation
Sermmai P., Tangthana-umrung K., Tailangka A., Rattanaburee T., Chompunud Na Ayudhya C., Dolsophon K., Tipmanee V., Graidist P., Thongpanchang T. Anticancer activity of the synthetic kusunokinin analogues on human cancer cell lines. Tetrahedron Vol.170 (2025). doi:10.1016/j.tet.2024.134362 Retrieved from: https://repository.li.mahidol.ac.th/handle/123456789/102808
item.page.dc.title
Anticancer activity of the synthetic kusunokinin analogues on human cancer cell lines
item.page.dc.contributor.author
item.page.oairecerif.author.affiliation
item.page.dc.contributor.correspondence
item.page.dc.contributor.other
item.page.dc.description.abstract
The series of racemic kusunokinin derivatives were synthesized and their cytotoxic activities and cell viability on cancer cells including breast cancer (MCF-7, MDA-MB468), colon cancer (HT-29), cholangiocarcinoma (KKU-M213) and ovarian cancer (A2780) cells were investigated. The results showed that compounds 6aa, 6da, and 6de exhibited growth inhibition against breast cancer (MDA-MB468), cholangiocarcinoma (KKU-M213), colon cancer (HT-29), and ovarian cancer (A2780) cells with IC50 values (μM) 13.77 ± 0.38, 7.94 ± 0.45, and 4.22 ± 0.13 (MDA-MB468); 4.21 ± 0.21, 0.97 ± 0.03, and 0.09 ± 0.02 (KKU-M213); 22.66 ± 0.23, and 15.62 ± 0.06 (HT-29); 13.11 ± 0.37, 11.51 ± 0.43, and 1.87 ± 0.01 (A2780); respectively. Interestingly, a positive control, doxorubicin, showed less cytotoxicity than 6da and 6de on cholangiocarcinoma KKU-M213 and ovarian cancer A2780 cells. Moreover, these three synthetic compounds also exhibited less toxicity than doxorubicin on the normal cells, MMNK-1, Vero and L-929. The binding possibility towards CSF1R, 6de (−11.59 kcal/mol) and trans-(−)-kusunokinin (−11.75 kcal/mol) were similar in both docking energies and docking poses. 6de interacted with Trp550 via π-π stacking in the similar manner with trans-(−)-kusunokinin and trans-(+)-kusunokinin.