RT Journal Article
T1 Novel phthalazin-1(2H)-one derivatives displaying a dithiocarbamate moiety as potential anticancer agents
A1 Vila Molares, Noemí
A1 Besada Pereira, Pedro
A1 Brea, José
A1 Loza, María Isabel
A1 Teran Moldes, Maria Del Carmen
K1 2302.22 Farmacología Molecular
K1 3209 Farmacología
K1 3207.03 Carcinogénesis
AB Nowadays, cancer disease seems to be the second most common cause of death worldwide. Molecular hybridization is a drug design strategy that has provided promising results against multifactorial diseases, including cancer. In this work, two series of phthalazinone-dithiocarbamate hybrids were described, compounds 6–8, which display the dithiocarbamate scaffold at N2, and compounds 9, in which this moiety was placed at C4. The proposed compounds were successfully synthesized via the corresponding aminoalkyl phthalazinone derivatives and using a one-pot reaction with carbon disulfide, anhydrous H3PO4, and different benzyl or propargyl bromides. The antiproliferative effects of the titled compounds were explored against three human cancer cell lines (A2780, NCI-H460, and MCF-7). The preliminary results revealed significant differences in activity and selectivity depending on the dithiocarbamate moiety location. Thus, in general terms, compounds 6–8 displayed better activity against the A-2780 and MCF-7 cell lines, while most of the analogues of the 9 group were selective toward the NCI-H460 cell line. Compounds 6e, 8e, 6g, 9a–b, 9d, and 9g with IC50 values less than 10 µM were the most promising. The drug-likeness and toxicity properties of the novel phthalazinone-dithiocarbamate hybrids were predicted using Swiss-ADME and ProTox web servers, respectively.
PB Molecules
SN 14203049
YR 2022
FD 2022-11-22
LK http://hdl.handle.net/11093/4151
UL http://hdl.handle.net/11093/4151
LA eng
NO Molecules, 27(23): 8115 (2022)
NO Universidade de Vigo, Xunta de Galicia | Ref. ED431C 2022/20
DS Investigo
RD 15-ene-2025