{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,5,14]],"date-time":"2026-05-14T01:29:19Z","timestamp":1778722159226,"version":"3.51.4"},"reference-count":23,"publisher":"Elsevier BV","license":[{"start":{"date-parts":[[2021,3,1]],"date-time":"2021-03-01T00:00:00Z","timestamp":1614556800000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/tdm\/userlicense\/1.0\/"},{"start":{"date-parts":[[2021,3,1]],"date-time":"2021-03-01T00:00:00Z","timestamp":1614556800000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/legal\/tdmrep-license"},{"start":{"date-parts":[[2021,3,1]],"date-time":"2021-03-01T00:00:00Z","timestamp":1614556800000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-017"},{"start":{"date-parts":[[2021,3,1]],"date-time":"2021-03-01T00:00:00Z","timestamp":1614556800000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-037"},{"start":{"date-parts":[[2021,3,1]],"date-time":"2021-03-01T00:00:00Z","timestamp":1614556800000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-012"},{"start":{"date-parts":[[2021,3,1]],"date-time":"2021-03-01T00:00:00Z","timestamp":1614556800000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-029"},{"start":{"date-parts":[[2021,3,1]],"date-time":"2021-03-01T00:00:00Z","timestamp":1614556800000},"content-version":"stm-asf","delay-in-days":0,"URL":"https:\/\/doi.org\/10.15223\/policy-004"}],"funder":[{"DOI":"10.13039\/100000002","name":"National Institutes of Health","doi-asserted-by":"publisher","id":[{"id":"10.13039\/100000002","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/100000060","name":"National Institute of Allergy and Infectious Diseases","doi-asserted-by":"publisher","id":[{"id":"10.13039\/100000060","id-type":"DOI","asserted-by":"publisher"}]},{"DOI":"10.13039\/501100001809","name":"National Natural Science Foundation of China","doi-asserted-by":"publisher","id":[{"id":"10.13039\/501100001809","id-type":"DOI","asserted-by":"publisher"}]}],"content-domain":{"domain":["elsevier.com","sciencedirect.com"],"crossmark-restriction":true},"short-container-title":["European Journal of Medicinal Chemistry"],"published-print":{"date-parts":[[2021,3]]},"DOI":"10.1016\/j.ejmech.2021.113202","type":"journal-article","created":{"date-parts":[[2021,1,21]],"date-time":"2021-01-21T22:14:11Z","timestamp":1611267251000},"page":"113202","update-policy":"https:\/\/doi.org\/10.1016\/elsevier_cm_policy","source":"Crossref","is-referenced-by-count":32,"special_numbering":"C","title":["Design and synthesis of mycobacterial pks13 inhibitors: Conformationally rigid tetracyclic molecules"],"prefix":"10.1016","volume":"213","author":[{"given":"Wei","family":"Zhang","sequence":"first","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Ling-ling","family":"Liu","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Shichun","family":"Lun","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Shuang-Shuang","family":"Wang","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Shiqi","family":"Xiao","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-3897-1948","authenticated-orcid":false,"given":"Hendra","family":"Gunosewoyo","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Fan","family":"Yang","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jie","family":"Tang","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-8734-4118","authenticated-orcid":false,"given":"William R.","family":"Bishai","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Li-Fang","family":"Yu","sequence":"additional","affiliation":[],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"78","reference":[{"key":"10.1016\/j.ejmech.2021.113202_bib1","series-title":"Global Tuberculosis Report 2018","author":"Who","year":"2018"},{"key":"10.1016\/j.ejmech.2021.113202_bib2","doi-asserted-by":"crossref","first-page":"325","DOI":"10.1016\/j.plipres.2012.05.002","article-title":"Towards understanding the functional diversity of cell wall mycolic acids of Mycobacterium tuberculosis","volume":"51","author":"Verschoor","year":"2012","journal-title":"Prog. Lipid Res."},{"key":"10.1016\/j.ejmech.2021.113202_bib3","doi-asserted-by":"crossref","first-page":"116","DOI":"10.1017\/S0031182016002377","article-title":"Mycobacterial cell wall biosynthesis: a multifaceted antibiotic target","volume":"145","author":"Abrahams","year":"2018","journal-title":"Parasitology"},{"key":"10.1016\/j.ejmech.2021.113202_bib4","doi-asserted-by":"crossref","first-page":"81","DOI":"10.1128\/CMR.18.1.81-101.2005","article-title":"Pathway to synthesis and processing of mycolic acids in Mycobacterium tuberculosis","volume":"18","author":"Takayama","year":"2005","journal-title":"Clin. Microbiol. Rev."},{"key":"10.1016\/j.ejmech.2021.113202_bib5","doi-asserted-by":"crossref","first-page":"1660","DOI":"10.1016\/j.chembiol.2014.10.011","article-title":"The polyketide synthase Pks13 catalyzes a novel mechanism of lipid transfer in mycobacteria","volume":"21","author":"Gavalda","year":"2014","journal-title":"Chem. Biol."},{"key":"10.1016\/j.ejmech.2021.113202_bib6","doi-asserted-by":"crossref","first-page":"499","DOI":"10.1038\/nchembio.1277","article-title":"Antituberculosis thiophenes define a requirement for Pks13 in mycolic acid biosynthesis","volume":"9","author":"Wilson","year":"2013","journal-title":"Nat. Chem. Biol."},{"key":"10.1016\/j.ejmech.2021.113202_bib7","doi-asserted-by":"crossref","first-page":"33675","DOI":"10.1074\/jbc.M111.325639","article-title":"Biochemical and structural study of the atypical acyltransferase domain from the mycobacterial polyketide synthase Pks13","volume":"287","author":"Bergeret","year":"2012","journal-title":"J.\u00a0Biol. Chem."},{"key":"10.1016\/j.ejmech.2021.113202_bib8","doi-asserted-by":"crossref","first-page":"19255","DOI":"10.1074\/jbc.M109.006940","article-title":"The Pks13\/FadD32 crosstalk for the biosynthesis of mycolic acids in Mycobacterium tuberculosis","volume":"284","author":"Gavalda","year":"2009","journal-title":"J.\u00a0Biol. Chem."},{"key":"10.1016\/j.ejmech.2021.113202_bib9","doi-asserted-by":"crossref","DOI":"10.1371\/journal.pone.0075245","article-title":"Identification of new drug targets and resistance mechanisms in Mycobacterium tuberculosis","volume":"8","author":"Ioerger","year":"2013","journal-title":"PloS One"},{"key":"10.1016\/j.ejmech.2021.113202_bib10","doi-asserted-by":"crossref","first-page":"249","DOI":"10.1016\/j.cell.2017.06.025","article-title":"Development of a novel lead that targets M. tuberculosis polyketide synthase 13","volume":"170","author":"Aggarwal","year":"2017","journal-title":"Cell"},{"key":"10.1016\/j.ejmech.2021.113202_bib11","doi-asserted-by":"crossref","first-page":"6119","DOI":"10.1039\/C6OB00821F","article-title":"Synthesis and evaluation of new 2-aminothiophenes against Mycobacterium tuberculosis","volume":"14","author":"Thanna","year":"2016","journal-title":"Org. Biomol. Chem."},{"key":"10.1016\/j.ejmech.2021.113202_bib12","doi-asserted-by":"crossref","first-page":"348","DOI":"10.1002\/anie.201709365","article-title":"An antibacterial beta-lactone kills Mycobacterium tuberculosis by disrupting mycolic acid biosynthesis","volume":"57","author":"Lehmann","year":"2018","journal-title":"Angew Chem. Int. Ed. Engl."},{"key":"10.1016\/j.ejmech.2021.113202_bib13","doi-asserted-by":"crossref","first-page":"791","DOI":"10.1021\/acs.jmedchem.7b01319","article-title":"Identification of novel coumestan derivatives as polyketide synthase 13 inhibitors against Mycobacterium tuberculosis","volume":"61","author":"Zhang","year":"2018","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2021.113202_bib14","doi-asserted-by":"crossref","first-page":"3575","DOI":"10.1021\/acs.jmedchem.9b00010","article-title":"Identification of novel coumestan derivatives as polyketide synthase 13 inhibitors against Mycobacterium tuberculosis. Part II","volume":"61","author":"Wei Zhang","year":"2019","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2021.113202_bib15","doi-asserted-by":"crossref","first-page":"2643","DOI":"10.1021\/ol9006663","article-title":"Simple conversion of enamines to 2H-azirines and their rearrangements under thermal conditions","volume":"11","author":"Li","year":"2009","journal-title":"Org. Lett."},{"key":"10.1016\/j.ejmech.2021.113202_bib16","doi-asserted-by":"crossref","first-page":"13575","DOI":"10.1002\/chem.201300389","article-title":"Aerobic iron-based cross-dehydrogenative coupling enables efficient diversity-oriented synthesis of coumestrol-based selective estrogen receptor modulators","volume":"19","author":"Kshirsagar","year":"2013","journal-title":"Chemistry"},{"key":"10.1016\/j.ejmech.2021.113202_bib17","doi-asserted-by":"crossref","first-page":"2266","DOI":"10.1021\/jm960858s","article-title":"Antitumor agents. 174. 2\u2019,3\u2019,4\u2019,5,6,7-Substituted 2-phenyl-1,8-naphthyridin-4-ones: their synthesis, cytotoxicity, and inhibition of tubulin polymerization","volume":"40","author":"Chen","year":"1997","journal-title":"J.\u00a0Med. Chem."},{"key":"10.1016\/j.ejmech.2021.113202_bib18","doi-asserted-by":"crossref","first-page":"3035","DOI":"10.1039\/b904188e","article-title":"Efficient copper-catalyzed coupling of aryl chlorides, bromides and iodides with aqueous ammonia","author":"Xu","year":"2009","journal-title":"Chem. Commun."},{"key":"10.1016\/j.ejmech.2021.113202_bib19","doi-asserted-by":"crossref","first-page":"5940","DOI":"10.1039\/C6OB01029F","article-title":"Cs2CO3 as a source of carbonyl and ethereal oxygen in a Cu-catalysed cascade synthesis of benzofuran [3,2-c] quinolin-6[5-H]ones","volume":"14","author":"Ali","year":"2016","journal-title":"Org. Biomol. Chem."},{"key":"10.1016\/j.ejmech.2021.113202_bib20","doi-asserted-by":"crossref","first-page":"334","DOI":"10.1002\/cmdc.201000490","article-title":"Pyrido[1,2-a]benzimidazole-based agents active against tuberculosis (TB), multidrug-resistant (MDR) TB and extensively drug-resistant (XDR) TB","volume":"6","author":"Pieroni","year":"2011","journal-title":"ChemMedChem"},{"key":"10.1016\/j.ejmech.2021.113202_bib21","doi-asserted-by":"crossref","first-page":"1004","DOI":"10.1128\/AAC.41.5.1004","article-title":"Microplate alamar blue assay versus BACTEC 460 system for high-throughput screening of compounds against Mycobacterium tuberculosis and Mycobacterium avium","volume":"41","author":"Collins","year":"1997","journal-title":"Antimicrob. Agents Chemother."},{"key":"10.1016\/j.ejmech.2021.113202_bib22","doi-asserted-by":"crossref","first-page":"2907","DOI":"10.1038\/ncomms3907","article-title":"Indoleamides are active against drug-resistant Mycobacterium tuberculosis","volume":"4","author":"Lun","year":"2013","journal-title":"Nat. Commun."},{"key":"10.1016\/j.ejmech.2021.113202_bib23","doi-asserted-by":"crossref","first-page":"424","DOI":"10.1016\/j.ejmech.2017.01.012","article-title":"The synthesis and antistaphylococcal activity of 9, 13-disubstituted berberine derivatives","volume":"127","author":"Wang","year":"2017","journal-title":"Eur. J. Med. Chem."}],"container-title":["European Journal of Medicinal Chemistry"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0223523421000519?httpAccept=text\/xml","content-type":"text\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S0223523421000519?httpAccept=text\/plain","content-type":"text\/plain","content-version":"vor","intended-application":"text-mining"}],"deposited":{"date-parts":[[2025,10,1]],"date-time":"2025-10-01T14:24:26Z","timestamp":1759328666000},"score":1,"resource":{"primary":{"URL":"https:\/\/linkinghub.elsevier.com\/retrieve\/pii\/S0223523421000519"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2021,3]]},"references-count":23,"alternative-id":["S0223523421000519"],"URL":"https:\/\/doi.org\/10.1016\/j.ejmech.2021.113202","relation":{},"ISSN":["0223-5234"],"issn-type":[{"value":"0223-5234","type":"print"}],"subject":[],"published":{"date-parts":[[2021,3]]},"assertion":[{"value":"Elsevier","name":"publisher","label":"This article is maintained by"},{"value":"Design and synthesis of mycobacterial pks13 inhibitors: Conformationally rigid tetracyclic molecules","name":"articletitle","label":"Article Title"},{"value":"European Journal of Medicinal Chemistry","name":"journaltitle","label":"Journal Title"},{"value":"https:\/\/doi.org\/10.1016\/j.ejmech.2021.113202","name":"articlelink","label":"CrossRef DOI link to publisher maintained version"},{"value":"article","name":"content_type","label":"Content Type"},{"value":"\u00a9 2021 Elsevier Masson SAS. All rights reserved.","name":"copyright","label":"Copyright"}],"article-number":"113202"}}