{"doi":"10.17615/bcc5-n195","title":"Design and synthesis of new 2-arylnaphthyridin-4-ones as potent antitumor agents targeting tumorigenic cell lines","abstract":"To develop new anticancer drug candidates from 2-arylnaphthyridin-4-one (AN), we have designed and synthesized a series of 3′-hydroxy and 6-hydroxy derivatives of AN. The results of cytotoxicity screening indicated that the replacement of the 3′-methoxy moiety on the C-ring phenyl group of AN (6a–e) with 3′-hydroxy (7a–e) made no significant effect on the inhibitory activity against HL-60, Hep3B and NCI-H460 cancer cell lines. On the other hand, replacing the 6-methoxy group on the A-ring of AN (6g–i) with a 6-hydroxy group (7g–i) resulted in reduced inhibitory activity against the above three cancer cell lines. Among the above-mentioned target compounds, 2-(3-hydroxyphenyl)-5-methyl-1,8-naphthyridin-4(1H)-one (7a) demonstrated the greatest potency and the best selectivity toward tumorigenic cancer cell lines. In a 7a preliminary mechanism of action study in Hep3B hepatoma cells, 7a showed the effects on microtubules followed by cell cycle arrest and sequentially led to apoptosis.","journal":"UNC Libraries","year":2020,"id":143049,"datarank":0.0,"base_score":0.0,"endowment":0.0,"self_citation_contribution":0.0,"citation_network_contribution":0.0,"self_endowment_contribution":0.0,"citer_contribution":0.0,"corpus_percentile":null,"corpus_rank":null,"citation_count":0,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":0,"is_dataset":false,"is_dataset_confidence":0.9471,"is_data_producer":false,"deposit_databanks":null,"is_oa":true,"file_count":0,"downloads":0,"has_version_chain":false,"published_date":"2020-01-01","fair_score":null,"fair_percentile":null,"algorithm_id":"datarank_citation_only_1hop_v6","ranking_scope":"data_only","authors":[{"id":548268,"name":"Ling‐Chu Chang","orcid":"0000-0002-7905-580X","position":1,"is_corresponding":false},{"id":610104,"name":"Yu Zhao","orcid":"0000-0002-2608-5044","position":2,"is_corresponding":false},{"id":26985,"name":"M. Tsai","orcid":"0000-0002-4728-9150","position":3,"is_corresponding":false},{"id":610671,"name":"Li-Chen Chou","orcid":null,"position":4,"is_corresponding":false},{"id":442798,"name":"Tian‐Shung Wu","orcid":null,"position":5,"is_corresponding":false},{"id":610672,"name":"Chih-Chang Liao","orcid":null,"position":6,"is_corresponding":false},{"id":547758,"name":"Li‐Jiau Huang","orcid":null,"position":7,"is_corresponding":false},{"id":467907,"name":"Hui‐Yi Lin","orcid":"0000-0002-3307-5549","position":8,"is_corresponding":false},{"id":153778,"name":"Yung-Yi Cheng","orcid":"0000-0001-7473-2835","position":9,"is_corresponding":false},{"id":244476,"name":"Kuo‐Hsiung Lee","orcid":"0000-0002-6562-0070","position":10,"is_corresponding":false},{"id":546987,"name":"Mei‐Hua Hsu","orcid":"0000-0003-2689-9774","position":11,"is_corresponding":false},{"id":610673,"name":"Yen-Fang Wen","orcid":null,"position":12,"is_corresponding":false},{"id":610105,"name":"Chi‐Hung Huang","orcid":"0000-0002-8887-4962","position":13,"is_corresponding":false},{"id":610106,"name":"Chin‐Yu Liu","orcid":"0009-0000-5318-1800","position":14,"is_corresponding":false},{"id":534548,"name":"Sheng‐Chu Kuo","orcid":null,"position":0,"is_corresponding":true}],"reference_count":0,"raw_metadata":null,"created_at":"2026-07-18T23:17:34.768426Z","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":[]}