TY - JOUR
T1 - Anticancer Effects of Novel Tetrahydro-Dimethyl-Xanthene-Diones
AU - Alagumuthu, Manikandan
AU - Arumugam, Siva Kumar
AU - Singh - Nee Nigam, Poonam
AU - Napoleon, Ayyakannu
PY - 2020/3/31
Y1 - 2020/3/31
N2 - Background: The derivatives of xanthene are known to have promising anticancer properties, in comparison to xanthene itself. Objective: The object of our study was to develop few xanthene derivatives (a family of fifteen novel 3,4,6,7-tetrahydro-3,3-dimethyl-9-phenyl-2H-xanthene-1,8(5H, 9H)-diones encoded as 4a-4m), which were effectively prepared through regioselective synthesis approach, and to test their anticancer effects. Methods: A series of cell lines were used in this study, first to assess the cytotoxicity and then the drug efficacy of target compounds, consecutively. Prior to MTT assay, the compounds were analysed for their antioxidant properties, since oxidative stress is an important factor in the development of many cancer types. The anticancer properties of 4a-m have been assessed over in silico (molecular docking and ADMET assessments) and in vitro (MTT assay) methods. Results: Compounds 4h and 4i showed a relative percentage anticancer activity of 86.25±1.25 & 89.74±1.64 against BT474 (ER+HER2+), and 90.56±1.18 & 93.24±1.80 against MCF-7 (ER-HER2), respectively. Conclusion: The animal model and pre-clinical studies for 4h and 4i should be performed in order to develop them as future anticancer agents.
AB - Background: The derivatives of xanthene are known to have promising anticancer properties, in comparison to xanthene itself. Objective: The object of our study was to develop few xanthene derivatives (a family of fifteen novel 3,4,6,7-tetrahydro-3,3-dimethyl-9-phenyl-2H-xanthene-1,8(5H, 9H)-diones encoded as 4a-4m), which were effectively prepared through regioselective synthesis approach, and to test their anticancer effects. Methods: A series of cell lines were used in this study, first to assess the cytotoxicity and then the drug efficacy of target compounds, consecutively. Prior to MTT assay, the compounds were analysed for their antioxidant properties, since oxidative stress is an important factor in the development of many cancer types. The anticancer properties of 4a-m have been assessed over in silico (molecular docking and ADMET assessments) and in vitro (MTT assay) methods. Results: Compounds 4h and 4i showed a relative percentage anticancer activity of 86.25±1.25 & 89.74±1.64 against BT474 (ER+HER2+), and 90.56±1.18 & 93.24±1.80 against MCF-7 (ER-HER2), respectively. Conclusion: The animal model and pre-clinical studies for 4h and 4i should be performed in order to develop them as future anticancer agents.
KW - Anticancer
KW - Antioxidant
KW - Cytotoxicity
KW - MTT assay
KW - Molecular docking
KW - Xanthene-diones
UR - https://pubmed.ncbi.nlm.nih.gov/32188389/?from_single_result=Anticancer+Effects+of+Novel+Tetrahydro-Dimethyl-Xanthene-Diones
UR - http://www.scopus.com/inward/record.url?scp=85086148378&partnerID=8YFLogxK
U2 - 10.2174/1871520620666200318094138
DO - 10.2174/1871520620666200318094138
M3 - Article
C2 - 32188389
SN - 1871-5206
VL - 20
SP - 909
EP - 916
JO - Anti-Cancer Agents in Medicinal Chemistry
JF - Anti-Cancer Agents in Medicinal Chemistry
IS - 7
ER -
