Please use this identifier to cite or link to this item: https://doi.org/10.1007/s10637-008-9205-5
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dc.titleSynthesis of novel 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole derivatives as antiproliferative agents: A structure-activity relationship study
dc.contributor.authorBenaka Prasad, S.B.
dc.contributor.authorVinaya, K.
dc.contributor.authorAnanda Kumar, C.S.
dc.contributor.authorSwarup, S.
dc.contributor.authorRangappa, K.S.
dc.date.accessioned2014-10-27T08:41:10Z
dc.date.available2014-10-27T08:41:10Z
dc.date.issued2009-12
dc.identifier.citationBenaka Prasad, S.B., Vinaya, K., Ananda Kumar, C.S., Swarup, S., Rangappa, K.S. (2009-12). Synthesis of novel 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole derivatives as antiproliferative agents: A structure-activity relationship study. Investigational New Drugs 27 (6) : 534-542. ScholarBank@NUS Repository. https://doi.org/10.1007/s10637-008-9205-5
dc.identifier.issn01676997
dc.identifier.urihttp://scholarbank.nus.edu.sg/handle/10635/101803
dc.description.abstractSummary: A series of novel 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole derivatives 5(a-m) were synthesized with different substituted aromatic/heterocyclic acid chlorides (R-CO-Cl) and characterized by 1H NMR, LC/MS, FTIR and elemental analyses. All the compounds synthesised were evaluated for their antiproliferative activity by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide (MTT) assay. The antiproliferative effects of the synthesised compounds were tested against viable human skin fibroblast cells and carcinoma cells namely HeLa cells, HT-29 cells, MCF-7 cells, HepG-2 cells by adopting positive and negative control. The importance of the aromatic and heterocyclic moiety was confirmed. From the SAR studies, it reveals that, the substitution at N-terminal of 6-fluoro-3-(4- piperidinyl)-1,2-benzisoxazole by the heterocyclic ring plays a dominant role and was responsible for the antiproliferative activity. Among the synthesized compounds 5a, 5d and 5k have showed potent antiproliferative activity on all the carcinoma cells tested. © 2008 Springer Science+Business Media, LLC.
dc.description.urihttp://libproxy1.nus.edu.sg/login?url=http://dx.doi.org/10.1007/s10637-008-9205-5
dc.sourceScopus
dc.subject2-benzisoxazole
dc.subject6-fluoro-3-(4-piperidinyl)-1
dc.subjectAcid chloride
dc.subjectAntiproliferative activity
dc.subjectCancer therapy
dc.subjectCell proliferation.
dc.subjectIsonipecotic acid
dc.subjectMTT assay
dc.typeArticle
dc.contributor.departmentBIOLOGICAL SCIENCES
dc.description.doi10.1007/s10637-008-9205-5
dc.description.sourcetitleInvestigational New Drugs
dc.description.volume27
dc.description.issue6
dc.description.page534-542
dc.description.codenINNDD
dc.identifier.isiut000271950500005
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