{"doi":"10.1016/j.bmc.2019.06.013","title":"Designed P-glycoprotein inhibitors with triazol-tetrahydroisoquinoline-core increase doxorubicin-induced mortality in multidrug resistant K562/A02 cells","abstract":null,"journal":"Bioorganic & Medicinal Chemistry","year":2019,"id":607934,"datarank":0.49983067652628066,"base_score":3.332204510175204,"endowment":3.332204510175204,"self_citation_contribution":0.49983067652628066,"citation_network_contribution":0.0,"self_endowment_contribution":0.49983067652628066,"citer_contribution":0.0,"corpus_percentile":null,"corpus_rank":null,"citation_count":27,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":null,"is_data_producer":false,"deposit_databanks":null,"is_oa":false,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":null,"fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":1561136,"name":"Qianqian Qiu","orcid":null,"position":1,"is_corresponding":false},{"id":1561138,"name":"Miaobo Pan","orcid":null,"position":2,"is_corresponding":false},{"id":425017,"name":"Qifei Li","orcid":"0000-0002-0069-8512","position":3,"is_corresponding":false},{"id":746005,"name":"Jiaqi Zhou","orcid":"0000-0001-6779-8297","position":4,"is_corresponding":false},{"id":1561139,"name":"Hesham Ghaleb","orcid":null,"position":5,"is_corresponding":false},{"id":1561140,"name":"Wenlong Huang","orcid":null,"position":6,"is_corresponding":false},{"id":500969,"name":"Hai Qian","orcid":"0000-0002-3827-0992","position":7,"is_corresponding":false},{"id":249393,"name":"Cheng Jiang","orcid":"0000-0003-4583-3295","position":8,"is_corresponding":false},{"id":1561134,"name":"Mutta Kairuki","orcid":null,"position":0,"is_corresponding":false}],"reference_count":0,"raw_metadata":{"has_enrichment":true,"resolved":true,"title":"Designed P-glycoprotein inhibitors with triazol-tetrahydroisoquinoline-core increase doxorubicin-induced mortality in multidrug resistant K562/A02 cells","abstract":"Multidrug resistance (MDR) refers to the cross-resistance of cancer cells to one drug, accompanied by other drugs with different mechanisms and structures, which is one of the main obstacles of clinical chemotherapy. Overexpression of P-glycoprotein (P-gp) was an extensively studied cause of MDR. Therefore, inhibiting P-gp have become an important strategy to reverse MDR. In this study, two series of triazole-tetrahydroisoquinoline-core P-gp inhibitors were designed and synthesized. Among them, compound I-5 had a remarkable reversal activity of MDR activity and the preliminary mechanism study was also carried out. All the results proved that compound I-5 was considered as a promising P-gp-mediated MDR reversal candidate.","is_dataset_classified":null,"base_score":0.0,"endowment":0.0,"datacite_reuse_total":0,"file_count":0,"downloads":0,"views":0,"has_version_chain":false,"is_dataset":false,"is_oa":false,"pmid":"31202598","pmcid":null,"openalex_id":null,"authors":[],"funders":[{"funder_name":"National Natural Science Foundation of China","grant_id":"","title":null}],"total_grants":1,"fwci":null,"citation_percentile":null,"influential_citations":0,"citation_trend":[],"oa_status":"closed","license":"https://www.elsevier.com/legal/tdmrep-license","oa_locations":[{"url":"https://api.elsevier.com/content/article/PII:S0968089619307758?httpAccept=text/xml","host_type":"publisher"},{"url":"https://api.elsevier.com/content/article/PII:S0968089619307758?httpAccept=text/plain","host_type":"publisher"}],"fields_of_study":[],"mesh_terms":["K562 Cells","Humans","Triazoles","Tetrahydroisoquinolines","Doxorubicin","Antibiotics, Antineoplastic","Drug Screening Assays, Antitumor","Drug Resistance, Multiple","Cell Survival","Molecular Structure","Structure-Activity Relationship","Dose-Response Relationship, Drug","Drug Design","Molecular Docking Simulation","ATP Binding Cassette Transporter, Subfamily B, Member 1"],"keywords":["Multidrug resistance","P-glycoprotein","K562/a02 Cells","Reversal Activity"],"sdg_mappings":[],"linked_datasets":[],"clinical_trials":[],"software_tools":[],"database_accessions":[],"source":"live","citation_network_status":"fetched"},"created_at":"2026-07-30T07:14:04.454579Z","pmid":null,"pmcid":null,"fwci":null,"citation_percentile":null,"influential_citations":0,"oa_status":null,"license":null,"views":0,"total_file_size_bytes":0,"version_count":0,"fair_f":null,"fair_a":null,"fair_i":null,"fair_r":null,"fair_zscore":null,"fair_rationale":null,"fair_model":null,"fair_agent_version":null,"fair_fulltext_source":null,"fair_has_llm":null,"fair_computed_at":null,"clinical_trials":[],"software_tools":[],"db_accessions":[],"linked_datasets":[],"topics":[]}