synthesis, cytotoxic and antimalarial activities of benzoyl thiosemicarbazone analogs of isoquinoline and related compounds合成、细胞毒性和抗疟活动thiosemicarbazone苯甲酰异喹啉和相关化合物的类似物.pdf

Molecules 2010, 15, 988-996; doi:10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article Synthesis, Cytotoxic and Antimalarial Activities of Benzoyl Thiosemicarbazone Analogs of Isoquinoline and Related Compounds 1, 1 2,3 Ratchanok Pingaew *, Supaluk Prachayasittikul , and Somsak Ruchirawat 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; E-Mail: ratchanok@swu.ac.th; Tel.: +662-649-5000 ext. 8222; Fax: +662-259-2097. Received: 13 January 2010; in revised form: 4 February 2010 / Accepted: 20 February 2010 / Published: 23 February 2010 Abstract: Thiosemicarbazone analogs of papaveraldine and related compounds 1–6 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 1–5 displayed cytotoxicity toward all the tested cell lines, while compounds 2–5 selectively showed potent activity against the MOLT-3