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Article: Synthesis and biological activity of fused furo[2,3-d] pyrimidinone derivatives as analgesic and antitumor agents

TitleSynthesis and biological activity of fused furo[2,3-d] pyrimidinone derivatives as analgesic and antitumor agents
Authors
KeywordsFused furo[2,3-d]pyrimidinone derivatives
Synthesis
Analgesic and antitumor
Issue Date2016
PublisherSpringer Netherlands. The Journal's web site is located at http://link.springer.com/journal/11164
Citation
Research on Chemical Intermediates, 2016, v. 42 n. 2, p. 939-949 How to Cite?
AbstractTumor growth is usually associated with persistent pain, especially during mid and terminal stages of cancer development. Nonetheless, a medicinal compound that possesses both anticancer and analgesic properties has not been identified. The 2-alkylthio-benzofuro[3,2-d]pyrimidin-4(3H)-ones (Code 5a–d) and 1-aryl-2-alkylthio-benzofuro[3,2-d]-1,2,4-triazolo[1,5-a]pyrimidin-5(1H)-ones (Code 10a–g) were synthesized by using the bioisostere concept, which were obtained via the aza-Wittig reaction of functionalized iminophosphoranes reacted with carbon disulfide and further reaction of the product with alkyl halides or halogenated aliphatic esters. The analgesic properties of 5a–d and 10a–g were studied using rat chronic constriction injury model and the antitumor properties of these chemicals were assessed using MTS cell proliferation assay. Results showed that 5a–d and 10a–g were found to attenuate thermal and mechanical allodynia induced by neuropathy and inhibited the proliferation of three human cancer cell lines (A459, HepG2, and HeLa). Among these compounds, 10g showed highly positive effects in both assessments, and would be selected for future work.
Persistent Identifierhttp://hdl.handle.net/10722/216725
ISSN
2023 Impact Factor: 2.8
2023 SCImago Journal Rankings: 0.476
ISI Accession Number ID

 

DC FieldValueLanguage
dc.contributor.authorLi, Q-
dc.contributor.authorChen, YM-
dc.contributor.authorHu, YG-
dc.contributor.authorLuo, X-
dc.contributor.authorKo, JKS-
dc.contributor.authorCheung, CW-
dc.date.accessioned2015-09-18T05:36:47Z-
dc.date.available2015-09-18T05:36:47Z-
dc.date.issued2016-
dc.identifier.citationResearch on Chemical Intermediates, 2016, v. 42 n. 2, p. 939-949-
dc.identifier.issn0922-6168-
dc.identifier.urihttp://hdl.handle.net/10722/216725-
dc.description.abstractTumor growth is usually associated with persistent pain, especially during mid and terminal stages of cancer development. Nonetheless, a medicinal compound that possesses both anticancer and analgesic properties has not been identified. The 2-alkylthio-benzofuro[3,2-d]pyrimidin-4(3H)-ones (Code 5a–d) and 1-aryl-2-alkylthio-benzofuro[3,2-d]-1,2,4-triazolo[1,5-a]pyrimidin-5(1H)-ones (Code 10a–g) were synthesized by using the bioisostere concept, which were obtained via the aza-Wittig reaction of functionalized iminophosphoranes reacted with carbon disulfide and further reaction of the product with alkyl halides or halogenated aliphatic esters. The analgesic properties of 5a–d and 10a–g were studied using rat chronic constriction injury model and the antitumor properties of these chemicals were assessed using MTS cell proliferation assay. Results showed that 5a–d and 10a–g were found to attenuate thermal and mechanical allodynia induced by neuropathy and inhibited the proliferation of three human cancer cell lines (A459, HepG2, and HeLa). Among these compounds, 10g showed highly positive effects in both assessments, and would be selected for future work.-
dc.languageeng-
dc.publisherSpringer Netherlands. The Journal's web site is located at http://link.springer.com/journal/11164-
dc.relation.ispartofResearch on Chemical Intermediates-
dc.subjectFused furo[2,3-d]pyrimidinone derivatives-
dc.subjectSynthesis-
dc.subjectAnalgesic and antitumor-
dc.titleSynthesis and biological activity of fused furo[2,3-d] pyrimidinone derivatives as analgesic and antitumor agents-
dc.typeArticle-
dc.identifier.emailCheung, CW: cheucw@hku.hk-
dc.identifier.authorityCheung, CW=rp00244-
dc.description.naturelink_to_subscribed_fulltext-
dc.identifier.doi10.1007/s11164-015-2064-8-
dc.identifier.scopuseid_2-s2.0-84929094473-
dc.identifier.hkuros252595-
dc.identifier.volume42-
dc.identifier.issue2-
dc.identifier.spage939-
dc.identifier.epage949-
dc.identifier.isiWOS:000371439000038-
dc.publisher.placeNetherlands-
dc.identifier.issnl0922-6168-

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