<abstract xmlns="http://www.w3.org/1999/xhtml"><p>Triazinopyrazolothieno pyrimidine derivatives <bold>1–5</bold> were evaluated for their anti-inflammatory, analgesic and anticancer activities and acute toxicity. Anti-inflammatory activity of the compounds was studied using the carrageenan test. All tested compounds showed analgesic activity, 3-methoxycarbonyl-4,6-dimethyl-8-[(<italic>N</italic>-methylindolyl)methyl] pyrimido [5′,4′:4,5]thieno [3′,2′-3,4]pyrazolo [5,1-<italic>c</italic>]triazine (<bold>4</bold>) showed activity comparable to that of diclofenac. Compounds <bold>1–5</bold> were also screened for anticancer activity on a human lung cancer cell line (A549) and a human prostate cancer cell line (DU145) using the MTT micro-cultured tetrazolium assay method. Compound <bold>4</bold> showed also significant anticancer activity against both cancer cell lines, comparable to that of doxorubicin. The most active compounds were tested for their acute toxicity and median lethal doses were evaluated.</p></abstract>

Triazinopyrazolothieno pyrimidine derivatives 1–5 were evaluated for their anti-inflammatory, analgesic and anticancer activities and acute toxicity. Anti-inflammatory activity of the compounds was studied using the carrageenan test. All tested compounds showed analgesic activity, 3-methoxycarbonyl-4,6-dimethyl-8-[(N-methylindolyl)methyl] pyrimido [5′,4′:4,5]thieno [3′,2′-3,4]pyrazolo [5,1-c]triazine (4) showed activity comparable to that of diclofenac. Compounds 1–5 were also screened for anticancer activity on a human lung cancer cell line (A549) and a human prostate cancer cell line (DU145) using the MTT micro-cultured tetrazolium assay method. Compound 4 showed also significant anticancer activity against both cancer cell lines, comparable to that of doxorubicin. The most active compounds were tested for their acute toxicity and median lethal doses were evaluated.

Pharmacological activities of some triazinopyrazolothieno pyrimidine derivatives

Faculty of Pharmacy, Department of Pharmacology and Toxicology

Acta Pharmaceutica

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

{"article-title":"Pharmacological activities of some triazinopyrazolothieno pyrimidine derivatives"}

Triazinopyrazolothieno pyrimidine derivatives 1–5 were evaluated for their anti-inflammatory, analgesic and anticancer activities and acute toxicity....

Pharmacological activities of some triazinopyrazolothieno pyrimidine derivatives

Publicado en línea: 30 ago 2017

Páginas: 407 - 414

Aceptado: 04 abr 2017

DOI: https://doi.org/10.1515/acph-2017-0022

Palabras clave
pyrimidine derivatives, triazinopyrazolothieno, anti-inflammatory, analgesic, anticancer, acute toxicity

© 2017 Saleh A. Bahashwan, published by De Gruyter Open

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Pharmacological activities of some triazinopyrazolothieno pyrimidine derivatives

Publicado en línea: 30 ago 2017

Páginas: 407 - 414

Aceptado: 04 abr 2017

DOI: https://doi.org/10.1515/acph-2017-0022

Palabras clavepyrimidine derivatives, triazinopyrazolothieno, anti-inflammatory, analgesic, anticancer, acute toxicity

© 2017 Saleh A. Bahashwan, published by De Gruyter Open

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Palabras clave
pyrimidine derivatives, triazinopyrazolothieno, anti-inflammatory, analgesic, anticancer, acute toxicity