{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,7]],"date-time":"2026-10-07T01:38:32Z","timestamp":1791337112581,"version":"4.3.1"},"reference-count":36,"publisher":"MDPI AG","issue":"10","license":[{"start":{"date-parts":[[2026,5,16]],"date-time":"2026-05-16T00:00:00Z","timestamp":1778889600000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"DOI":"10.13039\/501100006769","name":"Russian Science Foundation","doi-asserted-by":"publisher","award":["23-64-10018"],"award-info":[{"award-number":["23-64-10018"]}],"id":[{"id":"10.13039\/501100006769","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100006769","name":"Russian Science Foundation","doi-asserted-by":"publisher","award":["25-14-00305"],"award-info":[{"award-number":["25-14-00305"]}],"id":[{"id":"10.13039\/501100006769","id-type":"DOI","asserted-by":"publisher"}]},{"award":["23-64-10018"],"award-info":[{"award-number":["23-64-10018"]}],"id":[{"id":"https:\/\/ror.org\/03y2gwe85","id-type":"ROR","asserted-by":"publisher"}]},{"award":["25-14-00305"],"award-info":[{"award-number":["25-14-00305"]}],"id":[{"id":"https:\/\/ror.org\/03y2gwe85","id-type":"ROR","asserted-by":"publisher"}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["IJMS"],"abstract":"<jats:p>Quinazolinone derivatives are well-known anticancer agents; anticancer properties are also part of the broad spectrum of biological activity of coumarins. Conjugates containing quinazolin-4(3H)-one and coumarin fragments linked by polymethylene bridges of varying lengths were designed to improve properties of both parental compounds and create new anticancer or antibacterial agents. 3-{3-[(4-Methyl-2-oxo-2H-chromen-7-yl)oxy]propyl}quinazolin-4(3H)-one was synthesized as the base compound. It demonstrated moderate cytotoxicity against leukemia (K562 and HL60) and neuroblastoma (SH-SY5Y) cells in vitro, combined with relatively low acute, subacute, and chronic toxicity in vivo. Conjugates with various substituents and linkers were then synthesized to evaluate the structure\u2013activity relationship. A study of the synthesized compounds on cell cultures showed that the introduction of a methyl substituent into the benzene ring of the coumarin fragment led to both an increase in cytotoxicity and expansion of its spectrum of action. Testing of the hybrids against Gram-positive and Gram-negative bacteria revealed that the introduction of halogens into the quinazoline fragment in the compounds or the elongation of the linker led to the emergence of pronounced antibacterial properties, which were most clearly manifested against Acinetobacter baumanii. The possibility of directing activity of quinazoline-4(3H)-one\u2013coumarin hybrids by varying the substituents and the length of the linker was shown.<\/jats:p>","DOI":"10.3390\/ijms27104485","type":"journal-article","created":{"date-parts":[[2026,5,18]],"date-time":"2026-05-18T14:40:31Z","timestamp":1779115231000},"page":"4485","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":2,"title":["Synthesis and Biological Evaluation of New Quinazolin-4(3H)-One\u2013Coumarin Hybrids Designed as Anticancer and Antibacterial Agents"],"prefix":"10.3390","volume":"27","author":[{"given":"Maria P.","family":"Paramonova","sequence":"first","affiliation":[{"name":"Department of Pharmaceutical and Toxicological Chemistry, Volgograd State Medical University, Volgograd 400131, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Mikhail S.","family":"Novikov","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical and Toxicological Chemistry, Volgograd State Medical University, Volgograd 400131, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-0930-5604","authenticated-orcid":false,"given":"Vera A.","family":"Sokhraneva","sequence":"additional","affiliation":[{"name":"Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, Moscow 119991, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Iulia S.","family":"Zhivotova","sequence":"additional","affiliation":[{"name":"Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, Moscow 119991, Russia"},{"name":"Moscow Center for Advanced Studies, Moscow 123592, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Vasiliy A.","family":"Kezin","sequence":"additional","affiliation":[{"name":"Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, Moscow 119991, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0009-0005-7837-3856","authenticated-orcid":false,"given":"Martin A.","family":"Zenov","sequence":"additional","affiliation":[{"name":"Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, Moscow 119991, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-0787-415X","authenticated-orcid":false,"given":"Irina Yu.","family":"Petrushanko","sequence":"additional","affiliation":[{"name":"Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, Moscow 119991, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-9753-1881","authenticated-orcid":false,"given":"Olga N.","family":"Novikova","sequence":"additional","affiliation":[{"name":"Laboratory of Immunology, Federal State Unitary Enterprise \u201cResearch Institute of Hygiene, Toxicology, and Occupational Pathology\u201d of the Federal Medical and Biological Agency of the Russian Federation, Volgograd 400048, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-3272-4236","authenticated-orcid":false,"given":"Andrey V.","family":"Gorshenin","sequence":"additional","affiliation":[{"name":"Laboratory of Immunology, Federal State Unitary Enterprise \u201cResearch Institute of Hygiene, Toxicology, and Occupational Pathology\u201d of the Federal Medical and Biological Agency of the Russian Federation, Volgograd 400048, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yulia I.","family":"Velikorodnaya","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutical and Toxicological Chemistry, Volgograd State Medical University, Volgograd 400131, Russia"},{"name":"Laboratory of Immunology, Federal State Unitary Enterprise \u201cResearch Institute of Hygiene, Toxicology, and Occupational Pathology\u201d of the Federal Medical and Biological Agency of the Russian Federation, Volgograd 400048, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-3644-6966","authenticated-orcid":false,"given":"Elena B.","family":"Isakova","sequence":"additional","affiliation":[{"name":"Laboratory of Pharmacology and Chemotherapy, Gause Institute of New Antibiotics, Moscow 119021, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-6595-0811","authenticated-orcid":false,"given":"Andrey E.","family":"Shchekotikhin","sequence":"additional","affiliation":[{"name":"Laboratory of Chemical Transformation Antibiotic, Gause Institute of New Antibiotics, Moscow 119021, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-7443-6961","authenticated-orcid":false,"given":"Sergey N.","family":"Kochetkov","sequence":"additional","affiliation":[{"name":"Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, Moscow 119991, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-4981-7316","authenticated-orcid":false,"given":"Elena S.","family":"Matyugina","sequence":"additional","affiliation":[{"name":"Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, Moscow 119991, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-1452-0253","authenticated-orcid":false,"given":"Anastasia L.","family":"Khandazhinskaya","sequence":"additional","affiliation":[{"name":"Engelhardt Institute of Molecular Biology, Russian Academy of Sciences, Moscow 119991, Russia"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2026,5,16]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"877","DOI":"10.1007\/s40258-023-00824-6","article-title":"Projected Impact on Labour 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