Publication: Synthesis, cytotoxic and antimalarial activities of benzoyl thiosemicarbazone analogs of isoquinoline and related compounds
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Issued Date
2010
Resource Type
File Type
application/pdf
ISSN
14203049
Other identifier(s)
2-s2.0-77649206777
Rights Holder(s)
มหาวิทยาลัยศรีนครินทรวิโรฒ
Bibliographic Citation
Molecules. Vol 15, No.2 (2010), p.988-996
Suggested Citation
Pingaew R., Prachayasittikul S., Ruchirawat S. Synthesis, cytotoxic and antimalarial activities of benzoyl thiosemicarbazone analogs of isoquinoline and related compounds. Molecules. Vol 15, No.2 (2010), p.988-996. doi:10.3390/molecules15020988 Retrieved from: https://hdl.handle.net/20.500.14740/7620
Author(s)
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 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 thiosemicarbazones 3 and 4 showed antimalarial activity against Plasmodium falciparum with IC 50 of 10-7 to < 10-6 M. The study demonstrates the quite promising activity of analog 4 as a lead molecule for further development. © 2010 by the authors.
Subject(s)
Antimalarial agent
Antineoplastic agent
Isoquinoline derivative
Thiosemicarbazone derivative
Article
Cell death
Chemistry
Drug effect
Human
Plasmodium falciparum
Synthesis
Tumor cell line
Antimalarials
Antineoplastic Agents
Cell Death
Cell Line, Tumor
Humans
Isoquinolines
Plasmodium falciparum
Thiosemicarbazones
Antineoplastic agent
Isoquinoline derivative
Thiosemicarbazone derivative
Article
Cell death
Chemistry
Drug effect
Human
Plasmodium falciparum
Synthesis
Tumor cell line
Antimalarials
Antineoplastic Agents
Cell Death
Cell Line, Tumor
Humans
Isoquinolines
Plasmodium falciparum
Thiosemicarbazones