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

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.
Molecules 2010, 15(2), 988-996; https://doi.org/10.3390/molecules15020988
Received: 13 January 2010 / Revised: 4 February 2010 / Accepted: 20 February 2010 / Published: 23 February 2010
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. View Full-Text
Keywords: thiosemicarbazone; papaveraldine; cytotoxic activity; antimalarial activity thiosemicarbazone; papaveraldine; cytotoxic activity; antimalarial activity
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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. https://doi.org/10.3390/molecules15020988

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. https://doi.org/10.3390/molecules15020988

Chicago/Turabian Style

Pingaew, Ratchanok, Supaluk Prachayasittikul, and Somsak Ruchirawat. 2010. "Synthesis, Cytotoxic and Antimalarial Activities of Benzoyl Thiosemicarbazone Analogs of Isoquinoline and Related Compounds" Molecules 15, no. 2: 988-996. https://doi.org/10.3390/molecules15020988

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