{"doi":"10.1016/j.bmcl.2013.08.025","title":"Synthesis and SAR studies of 5-(pyridin-4-yl)-1,3,4-thiadiazol-2-amine derivatives as potent inhibitors of Bloom helicase","abstract":null,"journal":"Bioorganic & Medicinal Chemistry Letters","year":2013,"id":688623,"datarank":0.515098080672772,"base_score":3.4339872044851463,"endowment":3.4339872044851463,"self_citation_contribution":0.515098080672772,"citation_network_contribution":0.0,"self_endowment_contribution":0.515098080672772,"citer_contribution":0.0,"corpus_percentile":null,"corpus_rank":null,"citation_count":30,"citer_count":0,"citers_with_citation_signal":0,"citers_with_endowment":0,"datacite_reuse_total":1,"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":671060,"name":"Thomas S. 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In this work, we describe the medicinal chemistry optimization of the hit molecule following a quantitative high-throughput screen of >355,000 compounds. These efforts lead to the identification of ML216 and related analogs, which possess potent BLM inhibition and exhibit selectivity over related helicases. Moreover, these compounds demonstrated cellular activity by inducing sister chromatid exchanges, a hallmark of Bloom syndrome.","is_dataset_classified":null,"base_score":3.4339872044851463,"endowment":3.4339872044851463,"datacite_reuse_total":1,"file_count":0,"downloads":0,"views":0,"has_version_chain":false,"is_dataset":false,"is_oa":false,"pmid":"24012121","pmcid":"PMC3824626","openalex_id":"https://openalex.org/W2123391682","authors":[],"funders":[{"funder_name":"Molecular Libraries Initiative of the NIH Roadmap for Medical Research","grant_id":"U54MH084681","title":null},{"funder_name":"Molecular Libraries Initiative of the NIH Roadmap for Medical Research","grant_id":"R03MH087284","title":null},{"funder_name":"Wellcome Trust","grant_id":"092809","title":null},{"funder_name":"Wellcome Trust","grant_id":"092809/Z/10/Z","title":null},{"funder_name":"Intramural NIH HHS","grant_id":"Z99 TR999999","title":null},{"funder_name":"CIHR","grant_id":"","title":null},{"funder_name":"Cancer Research UK","grant_id":"","title":null}],"total_grants":7,"fwci":0.962,"citation_percentile":0.74940444,"influential_citations":0,"citation_trend":[{"year":2014,"count":4},{"year":2015,"count":1},{"year":2016,"count":2},{"year":2017,"count":4},{"year":2018,"count":2},{"year":2019,"count":1},{"year":2020,"count":3},{"year":2021,"count":6},{"year":2022,"count":2},{"year":2023,"count":1},{"year":2024,"count":3},{"year":2025,"count":1}],"oa_status":"green","license":"https://www.elsevier.com/legal/tdmrep-license","oa_locations":[{"url":"https://www.ncbi.nlm.nih.gov/pmc/articles/3824626","host_type":"repository"},{"url":"https://www.ncbi.nlm.nih.gov/pmc/articles/3824626","host_type":"repository"},{"url":"https://api.elsevier.com/content/article/PII:S0960894X13009542?httpAccept=text/xml","host_type":"publisher"},{"url":"https://api.elsevier.com/content/article/PII:S0960894X13009542?httpAccept=text/plain","host_type":"publisher"},{"url":"https://doi.org/10.1016/j.bmcl.2013.08.025","host_type":"journal"},{"url":"https://pubmed.ncbi.nlm.nih.gov/24012121","host_type":"repository"},{"url":"https://ora.ox.ac.uk/objects/uuid:0c462b9a-c6d6-410e-af28-6eaf78cad521","host_type":"repository"},{"url":"https://ora.ox.ac.uk/objects/uuid:8e1689ef-63c9-4292-b846-c7cbcfb0d932","host_type":"repository"},{"url":"https://researchprofiles.ku.dk/da/publications/1c6f215a-d609-4e3c-92d8-77785117a258","host_type":"repository"},{"url":"https://doi.org/10.7270/q2kk9d78","host_type":"repository"}],"fields_of_study":["DNA Repair Mechanisms","DNA and Nucleic Acid Chemistry","Carcinogens and Genotoxicity Assessment"],"mesh_terms":["Amines","Cell Membrane Permeability","Enzyme Inhibitors","Humans","Phenylurea Compounds","Structure-Activity Relationship","Thiadiazoles","Caco-2 Cells","RecQ Helicases"],"keywords":["Bloom syndrome","Helicase","Chemistry","DNA","RecQ helicase","DNA damage","DNA repair","Gene","Biochemistry","Genetics","Biology","RNA","Inhibitor","SAR","Structure activity relationship","SCE","NADPH","DMF","HTS","HR","Homologous Recombination","Dimethylformamide","Adme","Bs","Small Molecule","Nicotinamide Adenine Dinucleotide Phosphate","Sister Chromatid Exchanges","High Throughput Screen","Pbs","Phosphate Buffered Saline","Blm","Mlm","Absorption, Distribution, Metabolism And Excretion","Bloom Helicase","Peppsitm-ipr","[1,3-Bis(2,6-diisopropylphenyl)imidazole-2-ylidene](3-chloropyridyl)palladium(ii)chloride","Mouse Liver Microsomes"],"sdg_mappings":[{"sdg_number":0,"sdg_label":"Good health and well-being"}],"linked_datasets":[{"doi":"10.7270/q2kk9d78","title":"BindingDB Entry 50043401: Synthesis and SAR studies of 5-(pyridin-4-yl)-1,3,4-thiadiazol-2-amine derivatives as potent inhibitors of Bloom helicase.","publisher":"BindingDB","resource_type":"Dataset"}],"clinical_trials":[],"software_tools":[],"database_accessions":[],"source":"live","citation_network_status":"fetched"},"created_at":"2026-08-19T17:59:23.641047Z","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":[]}