{"id":{"repo_id":"uiuc","oai_identifier":"oai:www.ideals.illinois.edu:2142/110875"},"canonical_url":"https://search.dev.ndltd.org/etd/uiuc/oai:www.ideals.illinois.edu:2142/110875","repository":{"repo_id":"uiuc","name":"University of Illinois - Urbana-Champaign","base_url":"https://www.ideals.illinois.edu/oai-pmh"},"display":{"title":"Discovery of covalent modifiers via the complexity to diversity strategy","abstract":"Targeted covalent drugs have recently become integral parts of drug discovery. Given the advantages of high-throughput screening in drug discovery, many electrophilic fragment collections have been developed as a promising alternative to discover and validate novel targets. However, most covalent screening libraries consist of flat, low molecular weight compounds that are lacking in complexity and are incapable of addressing more complex targets, such as protein-protein interactions. To fill this gap, a library of 19 complex and diverse compounds containing electrophilic moieties has been synthesized and screened for anticancer activity in cell culture. The results from these studies suggest the potential for electrophilic natural product-like compounds to be used in the investigation of biological targets implicated in cancer.","abstract_html":"Targeted covalent drugs have recently become integral parts of drug discovery. Given the advantages of high-throughput screening in drug discovery, many electrophilic fragment collections have been developed as a promising alternative to discover and validate novel targets. However, most covalent screening libraries consist of flat, low molecular weight compounds that are lacking in complexity and are incapable of addressing more complex targets, such as protein-protein interactions. To fill this gap, a library of 19 complex and diverse compounds containing electrophilic moieties has been synthesized and screened for anticancer activity in cell culture. The results from these studies suggest the potential for electrophilic natural product-like compounds to be used in the investigation of biological targets implicated in cancer.","abstract_has_math":false,"creators":["Sawyer, Adam Michael"],"institution":"University of Illinois at Urbana-Champaign","degree_name":"M.S.","degree_level":"Thesis","degree_discipline":"Chemistry","degree_department":null,"school":null,"contributors":["Hergenrother, Paul J"],"advisors":[],"committee_chairs":[],"committee_members":[],"year":2021,"date_issued":"2021-04-29","date_published":"2021-04-29","updated_at":"2026-07-22T22:24:52Z","subjects":["Covalent modifiers","targeted covalent inhibitors","complexity to diversity","complex molecule synthesis"],"languages":["en"],"rights":["Copyright 2021 Adam Sawyer"],"rights_urls":[],"identifier_entries":[]},"links":{"outbound_url":"http://hdl.handle.net/2142/110875","outbound_label":"Handle","outbound_source":"dc:identifier"},"metadata_groups":[{"id":"people","label":"People","entries":[{"key":"dc:contributor","label":"Contributor","values":["Hergenrother, Paul J"]},{"key":"dc:creator","label":"Author","values":["Sawyer, Adam Michael"]}]},{"id":"academic_context","label":"Academic Context","entries":[{"key":"dc:date","label":"Dc Date","values":["2021-04-29","2023-09-17T04:07:01Z","2021-09-17T04:06:57Z","2021-05"]},{"key":"dc:type","label":"Dc Type","values":["text","Thesis"]},{"key":"thesis:degree_discipline","label":"Discipline","values":["Chemistry"]},{"key":"thesis:degree_level","label":"Degree Level","values":["Thesis"]},{"key":"thesis:degree_name","label":"Degree Name","values":["M.S."]},{"key":"thesis:institution_name","label":"Thesis Institution Name","values":["University of Illinois at Urbana-Champaign"]}]},{"id":"subjects_keywords","label":"Subjects and Keywords","entries":[{"key":"dc:subject","label":"Dc Subject","values":["Covalent modifiers","targeted covalent inhibitors","complexity to diversity","complex molecule synthesis"]}]},{"id":"language_rights","label":"Language and Rights","entries":[{"key":"dc:language","label":"Dc Language","values":["en"]},{"key":"dc:rights","label":"Dc Rights","values":["Copyright 2021 Adam Sawyer"]}]},{"id":"identifiers","label":"Identifiers","entries":[{"key":"dc:identifier","label":"Identifier","values":["http://hdl.handle.net/2142/110875"]}]},{"id":"additional","label":"Additional Metadata","entries":[{"key":"dc:description","label":"Description","values":["Targeted covalent drugs have recently become integral parts of drug discovery. Given the advantages of high-throughput screening in drug discovery, many electrophilic fragment collections have been developed as a promising alternative to discover and validate novel targets. However, most covalent screening libraries consist of flat, low molecular weight compounds that are lacking in complexity and are incapable of addressing more complex targets, such as protein-protein interactions. To fill this gap, a library of 19 complex and diverse compounds containing electrophilic moieties has been synthesized and screened for anticancer activity in cell culture. The results from these studies suggest the potential for electrophilic natural product-like compounds to be used in the investigation of biological targets implicated in cancer.","Submission published under a 24 month embargo labeled 'Closed Access', the embargo will last until 2023-05-01","The student, Adam Sawyer, accepted the attached license on 2021-04-29 at 11:33.","The student, Adam Sawyer, submitted this Thesis for approval on 2021-04-29 at 11:43.","This Thesis was approved for publication on 2021-04-29 at 17:13.","DSpace SAF Submission Ingestion Package generated from Vireo submission #16617 on 2021-09-16 at 20:14:46","Made available in DSpace on 2021-09-17T04:06:57Z (GMT). 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Given the advantages of high-throughput screening in drug discovery, many electrophilic fragment collections have been developed as a promising alternative to discover and validate novel targets. However, most covalent screening libraries consist of flat, low molecular weight compounds that are lacking in complexity and are incapable of addressing more complex targets, such as protein-protein interactions. To fill this gap, a library of 19 complex and diverse compounds containing electrophilic moieties has been synthesized and screened for anticancer activity in cell culture. 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