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Molecules 2010, 15(2), 988-996; doi:10.3390/molecules15020988
Article

Synthesis, Cytotoxic and Antimalarial Activities of Benzoyl Thiosemicarbazone Analogs of Isoquinoline and Related Compounds

1,* , 1 and 2,3
Received: 13 January 2010; in revised form: 4 February 2010 / Accepted: 20 February 2010 / Published: 23 February 2010
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Abstract: Thiosemicarbazone analogs of papaveraldine and related compounds 16 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 15 displayed cytotoxicity toward all the tested cell lines, while compounds 25 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 µg/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.
Keywords: thiosemicarbazone; papaveraldine; cytotoxic activity; antimalarial activity thiosemicarbazone; papaveraldine; cytotoxic activity; antimalarial activity
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

Pingaew, R.; Prachayasittikul, S.; Ruchirawat, S. Synthesis, Cytotoxic and Antimalarial Activities of Benzoyl Thiosemicarbazone Analogs of Isoquinoline and Related Compounds. Molecules 2010, 15, 988-996.

AMA Style

Pingaew R, Prachayasittikul S, Ruchirawat S. Synthesis, Cytotoxic and Antimalarial Activities of Benzoyl Thiosemicarbazone Analogs of Isoquinoline and Related Compounds. Molecules. 2010; 15(2):988-996.

Chicago/Turabian Style

Pingaew, Ratchanok; Prachayasittikul, Supaluk; Ruchirawat, Somsak. 2010. "Synthesis, Cytotoxic and Antimalarial Activities of Benzoyl Thiosemicarbazone Analogs of Isoquinoline and Related Compounds." Molecules 15, no. 2: 988-996.


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