Screening a Small Library of Xanthones for Antitumor Activity and Identification of a Hit Compound which Induces Apoptosis
AbstractOur previous work has described a library of thioxanthones designed to have dual activity as P-glycoprotein modulators and antitumor agents. Some of these compounds had shown a significant cell growth inhibitory activity towards leukemia cell lines, without affecting the growth of non-tumor human fibroblasts. However, their effect in cell lines derived from solid tumors has not been previously studied. The present work aimed at: (i) screening this small series of compounds from an in-house library, for their in vitro cell growth inhibitory activity in human tumor cell lines derived from solid tumors; and (ii) initiate a study of the effect of the most potent compound on apoptosis. The tumor cell growth inhibitory effect of 27 compounds was first analysed in different human tumor cell lines, allowing the identification of a hit compound, TXA1. Its hydrochloride salt TXA1·HCl was then synthesized, to improve solubility and bioavailability. Both TXA1 and TXA1·HCl inhibited the growth of MCF-7, NCI-H460, A375-C5, HeLa, 786-O, Caki-2 and AGS cell lines. The effect of TXA1·HCl in MCF-7 cells was found to be irreversible and was associated, at least in part, with an increase in cellular apoptosis. View Full-Text
- Supplementary File 1:
Supplementary (PDF, 1072 KB)
Scifeed alert for new publicationsNever miss any articles matching your research from any publisher
- Get alerts for new papers matching your research
- Find out the new papers from selected authors
- Updated daily for 49'000+ journals and 6000+ publishers
- Define your Scifeed now
Barbosa, J.; Lima, R.T.; Sousa, D.; Gomes, A.S.; Palmeira, A.; Seca, H.; Choosang, K.; Pakkong, P.; Bousbaa, H.; Pinto, M.M.; Sousa, E.; Vasconcelos, M.H.; Pedro, M. Screening a Small Library of Xanthones for Antitumor Activity and Identification of a Hit Compound which Induces Apoptosis. Molecules 2016, 21, 81.
Barbosa J, Lima RT, Sousa D, Gomes AS, Palmeira A, Seca H, Choosang K, Pakkong P, Bousbaa H, Pinto MM, Sousa E, Vasconcelos MH, Pedro M. Screening a Small Library of Xanthones for Antitumor Activity and Identification of a Hit Compound which Induces Apoptosis. Molecules. 2016; 21(1):81.Chicago/Turabian Style
Barbosa, João; Lima, Raquel T.; Sousa, Diana; Gomes, Ana S.; Palmeira, Andreia; Seca, Hugo; Choosang, Kantima; Pakkong, Pannee; Bousbaa, Hassan; Pinto, Madalena M.; Sousa, Emília; Vasconcelos, M. H.; Pedro, Madalena. 2016. "Screening a Small Library of Xanthones for Antitumor Activity and Identification of a Hit Compound which Induces Apoptosis." Molecules 21, no. 1: 81.
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.