Cargando…
Synthesis, Cytotoxic and Antimalarial Activities of Benzoyl Thiosemicarbazone Analogs of Isoquinoline and Related Compounds
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 t...
Autores principales: | , , |
---|---|
Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Molecular Diversity Preservation International
2010
|
Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6263187/ https://www.ncbi.nlm.nih.gov/pubmed/20335957 http://dx.doi.org/10.3390/molecules15020988 |
_version_ | 1783375241339207680 |
---|---|
author | Pingaew, Ratchanok Prachayasittikul, Supaluk Ruchirawat, Somsak |
author_facet | Pingaew, Ratchanok Prachayasittikul, Supaluk Ruchirawat, Somsak |
author_sort | Pingaew, Ratchanok |
collection | PubMed |
description | 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 IC(50) 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 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. |
format | Online Article Text |
id | pubmed-6263187 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2010 |
publisher | Molecular Diversity Preservation International |
record_format | MEDLINE/PubMed |
spelling | pubmed-62631872018-12-03 Synthesis, Cytotoxic and Antimalarial Activities of Benzoyl Thiosemicarbazone Analogs of Isoquinoline and Related Compounds Pingaew, Ratchanok Prachayasittikul, Supaluk Ruchirawat, Somsak Molecules Article 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 IC(50) 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 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. Molecular Diversity Preservation International 2010-02-23 /pmc/articles/PMC6263187/ /pubmed/20335957 http://dx.doi.org/10.3390/molecules15020988 Text en © 2010 by the authors; licensee Molecular Diversity Preservation International, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/). |
spellingShingle | Article Pingaew, Ratchanok Prachayasittikul, Supaluk Ruchirawat, Somsak Synthesis, Cytotoxic and Antimalarial Activities of Benzoyl Thiosemicarbazone Analogs of Isoquinoline and Related Compounds |
title | Synthesis, Cytotoxic and Antimalarial Activities of Benzoyl Thiosemicarbazone Analogs of Isoquinoline and Related Compounds |
title_full | Synthesis, Cytotoxic and Antimalarial Activities of Benzoyl Thiosemicarbazone Analogs of Isoquinoline and Related Compounds |
title_fullStr | Synthesis, Cytotoxic and Antimalarial Activities of Benzoyl Thiosemicarbazone Analogs of Isoquinoline and Related Compounds |
title_full_unstemmed | Synthesis, Cytotoxic and Antimalarial Activities of Benzoyl Thiosemicarbazone Analogs of Isoquinoline and Related Compounds |
title_short | Synthesis, Cytotoxic and Antimalarial Activities of Benzoyl Thiosemicarbazone Analogs of Isoquinoline and Related Compounds |
title_sort | synthesis, cytotoxic and antimalarial activities of benzoyl thiosemicarbazone analogs of isoquinoline and related compounds |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6263187/ https://www.ncbi.nlm.nih.gov/pubmed/20335957 http://dx.doi.org/10.3390/molecules15020988 |
work_keys_str_mv | AT pingaewratchanok synthesiscytotoxicandantimalarialactivitiesofbenzoylthiosemicarbazoneanalogsofisoquinolineandrelatedcompounds AT prachayasittikulsupaluk synthesiscytotoxicandantimalarialactivitiesofbenzoylthiosemicarbazoneanalogsofisoquinolineandrelatedcompounds AT ruchirawatsomsak synthesiscytotoxicandantimalarialactivitiesofbenzoylthiosemicarbazoneanalogsofisoquinolineandrelatedcompounds |