Repository logo
 
Publication

Design, synthesis and biological evaluation of Arylpiperazine-based novel Phthalimides: active inducers of testicular germ cell apoptosis

2016Journal article Open access
Simple item page
dc.contributor.authorSingh, Anil K.
dc.contributor.authorBhardwaj, Jitender K.
dc.contributor.authorOlival, Ana
dc.contributor.authorKumar, Yogesh
dc.contributor.authorPodder, Avijit
dc.contributor.authorMaheshwari, Ankur
dc.contributor.authorAgrawal, Renuka
dc.contributor.authorLatha, N.
dc.contributor.authorSingh, Brajendra K.
dc.contributor.authorTomás, Helena
dc.contributor.authorRodrigues, João
dc.contributor.authorKishan, Ram
dc.contributor.authorRupini, B.
dc.contributor.authorRathi, Brijesh
dc.date.accessioned2019-07-10T11:16:30Z
dc.date.available2019-07-10T11:16:30Z
dc.date.issued2016
dc.description.abstractUnderstanding of apoptosis or programmed cell death has provided the basis for novel therapeutics that has resulted in rationally designed anticancer strategies. Recently, inducers of apoptosis have been used in cancer therapy. In this work, we describe the role of chiral phthalimides functionalized with piperazines as potential apoptotic inducers. The listed twenty phthalimides were assessed for their in vitro apoptotic activity against testicular germ cells. All phthalimides showed a significant apoptotic response (∼39 to ∼68%). TUNEL assay and acridine orange fluorescence staining were carried out to investigate the molecular mechanisms responsible for the cell death. Phthalimides exhibited substantial apoptotic induction following the intrinsic pathway mechanism. Studies advocated that the apoptotic induction was mediated through caspase-9, caspase-3, JNK MAP kinase and tumor suppressor p53, which was accompanied by DNA fragmentation and nuclear condensation. Besides, the best five phthalimides regarding apoptotic action were evaluated for in vitro cytotoxic effects against CAL-72 and MCF-7 cancer cell lines. Compounds showed efficient killing of cancer cells. This discovery of functionalized phthalimides as apoptotic inducers would be highly valuable in understanding the mechanism of apoptosis at the molecular level and opens up new possibilities for therapeutic strategies.pt_PT
dc.description.versioninfo:eu-repo/semantics/publishedVersionpt_PT
dc.identifier.citationSingh, A. K., Bhardwaj, J. K., Olival, A., Kumar, Y., Podder, A., Maheshwari, A., ... & Rodrigues, J. (2016). Design, synthesis and biological evaluation of Arylpiperazine-based novel Phthalimides: active inducers of testicular germ cell apoptosis. Journal of Chemical Sciences, 128(8), 1245-1263.pt_PT
dc.identifier.doi10.1007/s12039-016-1122-0pt_PT
dc.identifier.issn0974-3626
dc.identifier.urihttp://hdl.handle.net/10400.13/2474
dc.language.isoengpt_PT
dc.peerreviewedyespt_PT
dc.publisherIndian Academy of Sciencespt_PT
dc.relationFabrication of large-area Epitaxial Graphene by Chemical Vapor Deposition for device applications
dc.subjectPhthalimidespt_PT
dc.subjectApoptosispt_PT
dc.subjectMolecular dockingpt_PT
dc.subjectAryl piperazinept_PT
dc.subjectCancer cellspt_PT
dc.subject.pt_PT
dc.subjectFaculdade de Ciências Exatas e da Engenhariapt_PT
dc.subjectCentro de Química da Madeira
dc.titleDesign, synthesis and biological evaluation of Arylpiperazine-based novel Phthalimides: active inducers of testicular germ cell apoptosispt_PT
dc.typejournal article
dspace.entity.typePublication
oaire.awardTitleFabrication of large-area Epitaxial Graphene by Chemical Vapor Deposition for device applications
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/5876-PPCDTI/PTDC%2FCTM-NAN%2F121108%2F2010/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/5876/PEst-OE%2FQUI%2FUI0674%2F2014/PT
oaire.citation.endPage1263pt_PT
oaire.citation.startPage1245pt_PT
oaire.citation.titleJournal of Chemical Sciencespt_PT
oaire.citation.volume128(8)pt_PT
oaire.fundingStream5876-PPCDTI
oaire.fundingStream5876
person.familyNameDias Olival
person.familyNameTomás
person.familyNameRodrigues
person.familyNameRathi
person.givenNameAna Cristina
person.givenNameHelena
person.givenNameJoão
person.givenNameBrijesh
person.identifier556975
person.identifier.ciencia-id6610-5EA1-D660
person.identifier.ciencia-id4D14-D31E-A8BE
person.identifier.ciencia-idA81C-620E-DD6A
person.identifier.orcid0000-0001-5461-5420
person.identifier.orcid0000-0002-7856-2041
person.identifier.orcid0000-0003-4552-1953
person.identifier.orcid0000-0003-2133-8847
person.identifier.ridB-9995-2019
person.identifier.ridE-5991-2010
person.identifier.ridB-6816-2008
person.identifier.scopus-author-id6508104177
person.identifier.scopus-author-id9233278800
person.identifier.scopus-author-id35734866000
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.nameFundação para a Ciência e a Tecnologia
project.funder.nameFundação para a Ciência e a Tecnologia
rcaap.rightsopenAccesspt_PT
rcaap.typearticlept_PT
relation.isAuthorOfPublication7a7f997e-61d9-4d66-8500-3f769cd211e4
relation.isAuthorOfPublication3a747114-6ab9-454b-985b-00cbf792e273
relation.isAuthorOfPublication53031fca-b2e7-4ce4-bda9-61e486da4547
relation.isAuthorOfPublicatione3b047a3-558a-4a2a-94f2-e6950ce10bf0
relation.isAuthorOfPublication.latestForDiscovery7a7f997e-61d9-4d66-8500-3f769cd211e4
relation.isProjectOfPublication54be8bbd-e2ab-48ad-a59e-8ac2b59b4af2
relation.isProjectOfPublicationec6bb904-b852-4300-a638-266ee44773f0
relation.isProjectOfPublication.latestForDiscoveryec6bb904-b852-4300-a638-266ee44773f0

Files

Original bundle
Now showing 1 - 1 of 1
Thumbnail Image
Name:
Design synthesis and biological evaluation of Arylpiperazine-based novel Phthalimides.pdf
Size:
7.18 MB
Format:
Adobe Portable Document Format
Download
License bundle
Now showing 1 - 1 of 1
No Thumbnail Available
Name:
license.txt
Size:
1.71 KB
Format:
Item-specific license agreed upon to submission
Description:
Download

Collections

Artigos em revistas internacionais