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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
1 Department of Chemistry, Faculty of Science, Srinakharinwirot University, Sukhumvit 23, Bangkok 10110, Thailand 2 Laboratory of Medicinal Chemistry, Chulabhorn Research Institute, Vipavadee-Rangsit Highway, Bangkok 10210, Thailand 3 Program in Chemical Biology, Chulabhorn Graduate Institute and the Center of Excellence on Environmental Health, Toxicology and Management of Chemicals, Vipavadee-Rangsit Highway, Bangkok 10210, Thailand
* Author to whom correspondence should be addressed.
Received: 13 January 2010 / Revised: 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 (CC BY 3.0).
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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.

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