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. Anti-inflammatory activity of the compounds was studied using the carrageenan test. All tested compounds showed analgesic activity, 3-methoxycarbonyl-...
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Language: | English |
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2017-09-01
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Series: | Acta Pharmaceutica |
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Online Access: | https://doi.org/10.1515/acph-2017-0022 |
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author | Bahashwan Saleh A. |
author_facet | Bahashwan Saleh A. |
author_sort | Bahashwan Saleh A. |
collection | DOAJ |
description | 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. |
format | Article |
id | doaj-art-3cb3174119ad44e69a1db9486448c967 |
institution | Kabale University |
issn | 1846-9558 |
language | English |
publishDate | 2017-09-01 |
publisher | Sciendo |
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series | Acta Pharmaceutica |
spelling | doaj-art-3cb3174119ad44e69a1db9486448c9672025-02-02T09:44:22ZengSciendoActa Pharmaceutica1846-95582017-09-0167340741410.1515/acph-2017-0022acph-2017-0022Pharmacological activities of some triazinopyrazolothieno pyrimidine derivativesBahashwan Saleh A.0Taibah University, Faculty of Pharmacy, Department of Pharmacology and Toxicology, Madinah Munawara, Saudi ArabiaTriazinopyrazolothieno 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.https://doi.org/10.1515/acph-2017-0022pyrimidine derivativestriazinopyrazolothienoanti-inflammatoryanalgesicanticanceracute toxicity |
spellingShingle | Bahashwan Saleh A. Pharmacological activities of some triazinopyrazolothieno pyrimidine derivatives Acta Pharmaceutica pyrimidine derivatives triazinopyrazolothieno anti-inflammatory analgesic anticancer acute toxicity |
title | Pharmacological activities of some triazinopyrazolothieno pyrimidine derivatives |
title_full | Pharmacological activities of some triazinopyrazolothieno pyrimidine derivatives |
title_fullStr | Pharmacological activities of some triazinopyrazolothieno pyrimidine derivatives |
title_full_unstemmed | Pharmacological activities of some triazinopyrazolothieno pyrimidine derivatives |
title_short | Pharmacological activities of some triazinopyrazolothieno pyrimidine derivatives |
title_sort | pharmacological activities of some triazinopyrazolothieno pyrimidine derivatives |
topic | pyrimidine derivatives triazinopyrazolothieno anti-inflammatory analgesic anticancer acute toxicity |
url | https://doi.org/10.1515/acph-2017-0022 |
work_keys_str_mv | AT bahashwansaleha pharmacologicalactivitiesofsometriazinopyrazolothienopyrimidinederivatives |