%0 Journal Article
%T Synthesis, Cytotoxic and Antimalarial Activities of Benzoyl Thiosemicarbazone Analogs of Isoquinoline and Related Compounds
%A Ratchanok Pingaew
%A Supaluk Prachayasittikul
%A Somsak Ruchirawat
%J Molecules
%D 2010
%I MDPI AG
%R 10.3390/molecules15020988
%X Thiosemicarbazone analogs of papaveraldine and related compounds 1¨C6 were synthesized and evaluated for cytotoxic and antimalarial activities. The cytotoxic activity was tested against HuCCA-1, HepG2, A549 and MOLT-3 human cancer cell lines. Thiosemicarbazones 1¨C5 displayed cytotoxicity toward all the tested cell lines, while compounds 2¨C5 selectively showed potent activity against the MOLT-3 cell lines. Significantly, N(4)-phenyl-2-benzoylpyridine thiosemicarbazone 4 exhibited the most potent activity against HuCCA-1, HepG2, A549 and MOLT-3 cell lines with IC50 values of 0.03, 4.75, 0.04 and 0.004 ¦Ìg/mL, respectively. In addition, 2-benzoylpyridine thio-semicarbazones 3 and 4 showed antimalarial activity against Plasmodium falciparum with IC50 of 10-7 to < 10-6 M. The study demonstrates the quite promising activity of analog 4 as a lead molecule for further development.
%K thiosemicarbazone
%K papaveraldine
%K cytotoxic activity
%K antimalarial activity
%U http://www.mdpi.com/1420-3049/15/2/988