{ "access": { "embargo": { "active": false, "reason": null }, "files": "public", "record": "public", "status": "open" }, "created": "2024-12-12T16:14:23.718210+00:00", "custom_fields": { "aperta:science_branches": [ { "id": "sub_41", "title": { "en": "Health Sciences > Pharmacy > Professional Sciences > Pharmaceutical Chemistry", "tr": "Sa\u011fl\u0131k Bilimleri > Eczac\u0131l\u0131k > Meslek Bilimleri > Farmas\u00f6tik Kimya" } } ] }, "deletion_status": { "is_deleted": false, "status": "P" }, "files": { "count": 1, "enabled": true, "entries": { "Supplementary Information.pdf": { "access": { "hidden": false }, "checksum": "md5:19d3f62dd8e7dc557ad657ae6bdee496", "ext": "pdf", "id": "7cf8712f-7f53-4f4a-a4d2-a925cb0d3f41", "key": "Supplementary Information.pdf", "links": { "content": "https://aperta.ulakbim.gov.tr/api/records/274116/files/Supplementary%20Information.pdf/content", "iiif_api": "https://aperta.ulakbim.gov.tr/api/iiif/record:274116:Supplementary%20Information.pdf/full/full/0/default.png", "iiif_base": "https://aperta.ulakbim.gov.tr/api/iiif/record:274116:Supplementary%20Information.pdf", "iiif_canvas": "https://aperta.ulakbim.gov.tr/api/iiif/record:274116/canvas/Supplementary%20Information.pdf", "iiif_info": "https://aperta.ulakbim.gov.tr/api/iiif/record:274116:Supplementary%20Information.pdf/info.json", "self": "https://aperta.ulakbim.gov.tr/api/records/274116/files/Supplementary%20Information.pdf" }, "metadata": null, "mimetype": "application/pdf", "size": 6835056, "storage_class": "L" } }, "order": [], "total_bytes": 6835056 }, "id": "274116", "is_draft": false, "is_published": true, "links": { "access": "https://aperta.ulakbim.gov.tr/api/records/274116/access", "access_grants": "https://aperta.ulakbim.gov.tr/api/records/274116/access/grants", "access_links": "https://aperta.ulakbim.gov.tr/api/records/274116/access/links", "access_request": "https://aperta.ulakbim.gov.tr/api/records/274116/access/request", "access_users": "https://aperta.ulakbim.gov.tr/api/records/274116/access/users", "archive": "https://aperta.ulakbim.gov.tr/api/records/274116/files-archive", "archive_media": "https://aperta.ulakbim.gov.tr/api/records/274116/media-files-archive", "communities": "https://aperta.ulakbim.gov.tr/api/records/274116/communities", "communities-suggestions": "https://aperta.ulakbim.gov.tr/api/records/274116/communities-suggestions", "draft": "https://aperta.ulakbim.gov.tr/api/records/274116/draft", "files": "https://aperta.ulakbim.gov.tr/api/records/274116/files", "latest": "https://aperta.ulakbim.gov.tr/api/records/274116/versions/latest", "latest_html": "https://aperta.ulakbim.gov.tr/records/274116/latest", "media_files": "https://aperta.ulakbim.gov.tr/api/records/274116/media-files", "parent": "https://aperta.ulakbim.gov.tr/api/records/274086", "parent_html": "https://aperta.ulakbim.gov.tr/records/274086", "preview_html": "https://aperta.ulakbim.gov.tr/records/274116?preview=1", "requests": "https://aperta.ulakbim.gov.tr/api/records/274116/requests", "reserve_doi": "https://aperta.ulakbim.gov.tr/api/records/274116/draft/pids/doi", "self": "https://aperta.ulakbim.gov.tr/api/records/274116", "self_html": "https://aperta.ulakbim.gov.tr/records/274116", "self_iiif_manifest": "https://aperta.ulakbim.gov.tr/api/iiif/record:274116/manifest", "self_iiif_sequence": "https://aperta.ulakbim.gov.tr/api/iiif/record:274116/sequence/default", "thumbnails": { "10": "https://aperta.ulakbim.gov.tr/api/iiif/record:274116:Supplementary%20Information.pdf/full/%5E10,/0/default.jpg", "100": "https://aperta.ulakbim.gov.tr/api/iiif/record:274116:Supplementary%20Information.pdf/full/%5E100,/0/default.jpg", "1200": "https://aperta.ulakbim.gov.tr/api/iiif/record:274116:Supplementary%20Information.pdf/full/%5E1200,/0/default.jpg", "250": "https://aperta.ulakbim.gov.tr/api/iiif/record:274116:Supplementary%20Information.pdf/full/%5E250,/0/default.jpg", "50": "https://aperta.ulakbim.gov.tr/api/iiif/record:274116:Supplementary%20Information.pdf/full/%5E50,/0/default.jpg", "750": "https://aperta.ulakbim.gov.tr/api/iiif/record:274116:Supplementary%20Information.pdf/full/%5E750,/0/default.jpg" }, "versions": "https://aperta.ulakbim.gov.tr/api/records/274116/versions" }, "media_files": { "count": 0, "enabled": false, "entries": {}, "order": [], "total_bytes": 0 }, "metadata": { "creators": [ { "affiliations": [ { "name": "Department of Molecular Biology and Genetics, Burdur Mehmet Akif Ersoy University, Burdur 15030, T\u00fcrkiye" } ], "person_or_org": { "family_name": "Halilibrahim CIFTCI", "identifiers": [ { "identifier": "0000-0002-9796-7669", "scheme": "orcid" } ], "name": "Halilibrahim CIFTCI", "type": "personal" } }, { "affiliations": [ { "name": "Medicinal and Biological Chemistry Science Farm Joint Research Laboratory, Faculty of Life Sciences, Kumamoto University, Kumamoto 862-0973, Japan" } ], "person_or_org": { "family_name": "Masami OTSUKA", "identifiers": [ { "identifier": "0000-0002-2968-3939", "scheme": "orcid" } ], "name": "Masami OTSUKA", "type": "personal" } }, { "affiliations": [ { "name": "Medicinal and Biological Chemistry Science Farm Joint Research Laboratory, Faculty of Life Sciences, Kumamoto University, Kumamoto 862-0973, Japan" } ], "person_or_org": { "family_name": "Mikako FUJITA", "identifiers": [ { "identifier": "0000-0001-6705-4052", "scheme": "orcid" } ], "name": "Mikako FUJITA", "type": "personal" } }, { "affiliations": [ { "name": "Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, Eskisehir 26470, T\u00fcrkiye" } ], "person_or_org": { "family_name": "Belgin SEVER", "identifiers": [ { "identifier": "0000-0003-4847-9711", "scheme": "orcid" } ], "name": "Belgin SEVER", "type": "personal" } } ], "description": "

Epidermal growth factor receptor (EGFR) and HER2, pioneer members of the receptor tyrosine kinase subfamily, are frequently mutated and/or overexpressed in several types of human cancers, including non-small cell lung cancer (NSCLC) and breast cancer, which are leading causes of cancer-related deaths worldwide.  EGFR and HER2-focused anti-NSCLC and anti-breast cancer studies encouraged us to search for new potential agents. For this purpose, in the current work, naphthalene-linked pyrazoline-thiazole hybrids (BTT1-10 and BTP1-10) were synthesized and examined for their antiproliferative effects on A549 NSCLC and MCF-7 breast cancer cell lines. According to the results, MTT assay showed that BTT-5 induced strong toxicity in A549 cells with the IC50 value of 9.51±3.35 μM compared to lapatinib (IC50 = 16.44±3.92 μM). BTT-5 also presented a high selectivity profile between Jurkat cell line and PBMCs (healthy) (SI= 65.65). Furthermore, BTT-5 augmented apoptosis significantly in A549 cells (18.40%). BTT-5 displayed significant EGFR inhibition (58.32%) and no significant HER2 inhibition at 10 μM concentration interpreting its selective kinase inhibitory effects. Molecular docking assessment indicated that BTT-5 showed high affinity with a different binding profile than lapatinib in the ATP binding cleft of EGFR. Consequently, BTT-5 can serve as a lead for future anti-NSCLC studies.

", "publication_date": "2024-11-20", "resource_type": { "id": "other", "title": { "en": "Other", "tr": "Di\u011fer" } }, "rights": [ { "description": { "en": "" }, "icon": "cc-by-nc-icon", "id": "cc-by-nc-4.0", "props": { "scheme": "spdx", "url": "https://creativecommons.org/licenses/by-nc/4.0/legalcode" }, "title": { "en": "Creative Commons Attribution Non Commercial 4.0 International" } } ], "subjects": [ { "subject": "Naphthalene" }, { "subject": "Pyrazoline" }, { "subject": "Thiazole" }, { "subject": "EGFR" }, { "subject": "NSCLC" }, { "subject": "Breast cancer" } ], "title": "Supplementary Information" }, "parent": { "access": { "owned_by": { "user": "2512" } }, "communities": {}, "id": "274086", "pids": { "doi": { "identifier": "10.48623/aperta.274086", "provider": "datacite" } } }, "pids": { "doi": { "identifier": "10.48623/aperta.274116", "provider": "dummy" }, "oai": { "identifier": "oai:aperta.ulakbim.gov.tr:274116", "provider": "oai" } }, "revision_id": 2, "stats": { "all_versions": { "data_volume": 1909812942.0, "downloads": 287, "unique_downloads": 278, "unique_views": 1261, "views": 1261 }, "this_version": { "data_volume": 444278640.0, "downloads": 65, "unique_downloads": 63, "unique_views": 96, "views": 96 } }, "status": "published", "swh": {}, "updated": "2024-12-18T07:44:50.287663+00:00", "versions": { "index": 2, "is_latest": false } }