{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,17]],"date-time":"2026-09-17T02:41:22Z","timestamp":1789612882673,"version":"build-2803163510"},"reference-count":40,"publisher":"Elsevier BV","issue":"3","license":[{"start":{"date-parts":[[2020,3,1]],"date-time":"2020-03-01T00:00:00Z","timestamp":1583020800000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/tdm\/userlicense\/1.0\/"},{"start":{"date-parts":[[2020,3,1]],"date-time":"2020-03-01T00:00:00Z","timestamp":1583020800000},"content-version":"tdm","delay-in-days":0,"URL":"https:\/\/www.elsevier.com\/legal\/tdmrep-license"},{"start":{"date-parts":[[2019,8,29]],"date-time":"2019-08-29T00:00:00Z","timestamp":1567036800000},"content-version":"vor","delay-in-days":0,"URL":"http:\/\/creativecommons.org\/licenses\/by-nc-nd\/4.0\/"}],"funder":[{"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":["Acta Pharmaceutica Sinica B"],"published-print":{"date-parts":[[2020,3]]},"DOI":"10.1016\/j.apsb.2019.08.009","type":"journal-article","created":{"date-parts":[[2019,9,5]],"date-time":"2019-09-05T12:24:21Z","timestamp":1567686261000},"page":"512-528","update-policy":"https:\/\/doi.org\/10.1016\/elsevier_cm_policy","source":"Crossref","is-referenced-by-count":42,"title":["Synthesis and biological evaluation of a series of 2-(((5-akly\/aryl-1H-pyrazol-3-yl)methyl)thio)-5-alkyl-6-(cyclohexylmethyl)-pyrimidin-4(3H)-ones as potential HIV-1 inhibitors"],"prefix":"10.1016","volume":"10","author":[{"given":"Yumeng","family":"Wu","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Chengrun","family":"Tang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ruomei","family":"Rui","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Liumeng","family":"Yang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Wei","family":"Ding","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jiangyuan","family":"Wang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yiming","family":"Li","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Christopher C.","family":"Lai","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yueping","family":"Wang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Ronghua","family":"Luo","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Weilie","family":"Xiao","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Hongbing","family":"Zhang","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yongtang","family":"Zheng","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yanping","family":"He","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"78","reference":[{"key":"10.1016\/j.apsb.2019.08.009_bib1","doi-asserted-by":"crossref","first-page":"25","DOI":"10.1016\/j.antiviral.2009.10.007","article-title":"Current status and challenges of antiretroviral research and therapy","volume":"85","author":"Est\u00e9","year":"2010","journal-title":"Antivir Res"},{"key":"10.1016\/j.apsb.2019.08.009_bib2","doi-asserted-by":"crossref","first-page":"230","DOI":"10.1097\/COH.0b013e32835ef089","article-title":"Combined approaches for HIV cure","volume":"8","author":"Margolis","year":"2013","journal-title":"Curr Opin HIV AIDS"},{"key":"10.1016\/j.apsb.2019.08.009_bib3","doi-asserted-by":"crossref","first-page":"1295","DOI":"10.1126\/science.278.5341.1295","article-title":"Identification of a reservoir for HIV-1 in patients on highly active antiretroviral therapy","volume":"278","author":"Finzi","year":"1997","journal-title":"Science"},{"key":"10.1016\/j.apsb.2019.08.009_bib4","doi-asserted-by":"crossref","first-page":"359","DOI":"10.2174\/092986711794839142","article-title":"Recent advances in DAPYs and related analogues as HIV-1 NNRTIs","volume":"18","author":"Chen","year":"2011","journal-title":"Curr Med Chem"},{"key":"10.1016\/j.apsb.2019.08.009_bib5","doi-asserted-by":"crossref","first-page":"2186","DOI":"10.2174\/092986711795656180","article-title":"Twenty years of HIV-1 non-nucleoside reverse transcriptase inhibitors: time to reevaluate their toxicity","volume":"18","author":"Blas-Garcia","year":"2011","journal-title":"Curr Med Chem"},{"key":"10.1016\/j.apsb.2019.08.009_bib6","doi-asserted-by":"crossref","first-page":"1087","DOI":"10.1517\/14656566.2013.787411","article-title":"Etravirine for the treatment of HIV\/AIDS","volume":"14","author":"Schrijvers","year":"2013","journal-title":"Expert Opin Pharmacother"},{"key":"10.1016\/j.apsb.2019.08.009_bib7","doi-asserted-by":"crossref","first-page":"253","DOI":"10.1097\/COH.0000000000000160","article-title":"Long-acting rilpivirine for HIV prevention","volume":"10","author":"Jackson","year":"2015","journal-title":"Curr Opin HIV AIDS"},{"key":"10.1016\/j.apsb.2019.08.009_bib8","doi-asserted-by":"crossref","first-page":"215","DOI":"10.1016\/j.ejmech.2015.08.007","article-title":"Pyrimidine sulfonylacetanilides with improved potency against key mutant viruses of HIV-1 by specific targeting of a highly conserved residue","volume":"102","author":"Wan","year":"2015","journal-title":"Eur J Med Chem"},{"key":"10.1016\/j.apsb.2019.08.009_bib9","doi-asserted-by":"crossref","first-page":"2876","DOI":"10.2174\/092986709788803231","article-title":"Recent advances in the discovery and development of novel HIV-1 NNRTI platforms: 2006\u20132008 update","volume":"16","author":"Zhan","year":"2009","journal-title":"Curr Med Chem"},{"key":"10.1016\/j.apsb.2019.08.009_bib10","doi-asserted-by":"crossref","first-page":"329","DOI":"10.2174\/09298673113206660298","article-title":"Recent advances in the discovery and development of novel HIV-1 NNRTI platforms (Part II): 2009\u20132013 update","volume":"21","author":"Song","year":"2014","journal-title":"Curr Med Chem"},{"key":"10.1016\/j.apsb.2019.08.009_bib11","doi-asserted-by":"crossref","first-page":"717","DOI":"10.1517\/13543776.2011.568481","article-title":"Novel HIV-1 non-nucleoside reverse transcriptase inhibitors: a patent review (2005\u22122010)","volume":"21","author":"Zhan","year":"2011","journal-title":"Expert Opin Ther Pat"},{"key":"10.1016\/j.apsb.2019.08.009_bib12","doi-asserted-by":"crossref","first-page":"3595","DOI":"10.1021\/jm200990c","article-title":"Strategies for the design of HIV-1 non-nucleoside reverse transcriptase inhibitors: lessons from the development of seven representative paradigms","volume":"55","author":"Li","year":"2012","journal-title":"J Med Chem"},{"key":"10.1016\/j.apsb.2019.08.009_bib13","doi-asserted-by":"crossref","first-page":"2849","DOI":"10.1021\/acs.jmedchem.5b00497","article-title":"Anti-HIV drug discovery and development: current innovations and future trends","volume":"59","author":"Zhan","year":"2016","journal-title":"J Med Chem"},{"key":"10.1016\/j.apsb.2019.08.009_bib14","doi-asserted-by":"crossref","first-page":"361","DOI":"10.1177\/095632029300400608","article-title":"3,4-Dihydro-2-alkoxy-6-benzyl-4-oxopyrimidines (DABOs): a new class of specific inhibitors of human immunodeficiency virus type 1","volume":"4","author":"Artico","year":"1993","journal-title":"Antiviral Chem Chemother"},{"key":"10.1016\/j.apsb.2019.08.009_bib15","doi-asserted-by":"crossref","first-page":"329","DOI":"10.1080\/14756360600774413","article-title":"Novel tight binding PETT, HEPT and DABO-based non-nucleoside inhibitors of HIV-1 reverse transcriptase","volume":"21","author":"D\u2019cruz","year":"2006","journal-title":"J Enzyme Inhib Med Chem"},{"key":"10.1016\/j.apsb.2019.08.009_bib16","doi-asserted-by":"crossref","first-page":"619","DOI":"10.1021\/jm980260f","article-title":"5-Alkyl-2-(alkylthio)-6-(2,6-dihalophenylmethyl)-3,4-dihydropyrimidin-4(3H)-ones: novel potent and selective dihydro-alkoxy-benzyl-oxopyrimidine derivatives","volume":"42","author":"Mai","year":"1999","journal-title":"J Med Chem"},{"key":"10.1016\/j.apsb.2019.08.009_bib17","doi-asserted-by":"crossref","first-page":"4641","DOI":"10.1021\/jm800340w","article-title":"5-Alkyl-6-benzyl-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones, a series of anti-HIV-1 agents of the dihydro-alkoxy-benzyl-oxopyrimidine family with peculiar structure-activity relationship profile","volume":"51","author":"Nawrozkij","year":"2008","journal-title":"J Med Chem"},{"key":"10.1016\/j.apsb.2019.08.009_bib18","doi-asserted-by":"crossref","first-page":"1016","DOI":"10.1016\/j.ejmech.2008.06.028","article-title":"Synthesis and in\u00a0vitro anti-HIV evaluation of a new series of 6-arylmethyl-substituted S-DABOs as potential non-nucleoside HIV-1 reverse transcriptase inhibitors","volume":"44","author":"Wang","year":"2009","journal-title":"Eur J Med Chem"},{"key":"10.1016\/j.apsb.2019.08.009_bib19","doi-asserted-by":"crossref","first-page":"152","DOI":"10.2174\/092986712803414169","article-title":"Dihydro-alkoxyl-benzyl-oxopyrimidine derivatives (DABOs) as non-nucleoside reverse transcriptase inhibitors: an update review (2001\u20132011)","volume":"19","author":"Yang","year":"2012","journal-title":"Curr Med Chem"},{"key":"10.1016\/j.apsb.2019.08.009_bib20","doi-asserted-by":"crossref","first-page":"2376","DOI":"10.2174\/092986711795843209","article-title":"Recent advances in the DABOs family as potent HIV-1 non-nucleoside reverse transcriptase inhibitors","volume":"18","author":"Yu","year":"2011","journal-title":"Curr Med Chem"},{"key":"10.1016\/j.apsb.2019.08.009_bib21","first-page":"3173","article-title":"5-Alkyl-2-[(aryl and alkyloxylcarbonylmethyl)thio]-6-(1-naphthylmethyl) pyrimidin-4(3H)-ones as an unique HIV reverse transcriptase inhibitors\u00a0of S-DABO series","volume":"14","author":"He","year":"2004","journal-title":"Bioorg Med Chem Lett"},{"key":"10.1016\/j.apsb.2019.08.009_bib22","doi-asserted-by":"crossref","first-page":"536","DOI":"10.1016\/j.bioorg.2004.05.007","article-title":"Nonnucleoside HIV-1 reverse transcriptase inhibitors; Part 3. Synthesis and antiviral activity of 5-alkyl-2-[(aryl and alkyloxyl-carbonylmethyl)thio]-6-(1-naphthylmethyl) pyrimidin-4(3H)-ones","volume":"32","author":"He","year":"2004","journal-title":"Bioorg Chem"},{"key":"10.1016\/j.apsb.2019.08.009_bib23","first-page":"228","article-title":"The anti-HIV activity of three 2-alkylsulfanyl-6-benzyl-3,4-dihydropyrimidin-4(3H)-one derivatives acting as non-nucleoside reverse transcriptase inhibitor in\u00a0vitro","volume":"45","author":"Long","year":"2010","journal-title":"Acta Pharm Sin"},{"key":"10.1016\/j.apsb.2019.08.009_bib24","doi-asserted-by":"crossref","first-page":"967","DOI":"10.1007\/s00706-007-0834-8","article-title":"Synthesis and anti-HIV-1 activity of S-dihydro(alkyloxy)benzyloxypyrimidine derivatives","volume":"139","author":"Rao","year":"2008","journal-title":"Monatsh Chem"},{"key":"10.1016\/j.apsb.2019.08.009_bib25","doi-asserted-by":"crossref","first-page":"694","DOI":"10.1016\/j.bmcl.2010.12.003","article-title":"Synthesis and biological evaluation of novel dihydro-aryl\/alkylsulfanyl-cyclohexylmethyl-oxopyrimidines (S-DACOs) as high active anti-HIV agents","volume":"21","author":"He","year":"2011","journal-title":"Bioorg Med Chem Lett"},{"key":"10.1016\/j.apsb.2019.08.009_bib26","article-title":"DB-02, a C-6-cyclohexylmethyl substituted pyrimidinone HIV-1 reverse transcriptase inhibitor with nanomolar activity, displays an improved sensitivity against K103N or Y181C than S-DABOs","volume":"11","author":"Zhang","year":"2013","journal-title":"PLoS One"},{"key":"10.1016\/j.apsb.2019.08.009_bib27","first-page":"271","article-title":"Synthesis\u00a0and biological evaluation of novel hydroxylphenethyl-S-DACOs as high active anti-HIV agents","volume":"10","author":"Wu","year":"2013","journal-title":"Lett Drug Des Discov"},{"key":"10.1016\/j.apsb.2019.08.009_bib28","doi-asserted-by":"crossref","first-page":"290","DOI":"10.1055\/s-1993-25849","article-title":"A safe, economical method for the preparation of \u03b2-oxo esters","volume":"1993","author":"Clay","year":"1993","journal-title":"Synthesis"},{"key":"10.1016\/j.apsb.2019.08.009_bib29","doi-asserted-by":"crossref","first-page":"2675","DOI":"10.1021\/ol060570p","article-title":"1,3-Diketones from acid chlorides and ketones: a rapid and general one-pot synthesis of pyrazoles","volume":"8","author":"Heller","year":"2006","journal-title":"Org Lett"},{"key":"10.1016\/j.apsb.2019.08.009_bib30","doi-asserted-by":"crossref","first-page":"4366","DOI":"10.1016\/j.bmc.2011.05.024","article-title":"Synthesis and biological evaluation of novel 5-alkyl-2-arylthio-6-((3,4-dihydroquinolin-1(2H)-yl)methyl)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors","volume":"19","author":"Zhang","year":"2011","journal-title":"Bioorg Med Chem"},{"key":"10.1016\/j.apsb.2019.08.009_bib31","first-page":"30","article-title":"Does the 2-methylthiomethyl substituent really confer high anti-HIV-1 activity to S-DABOs?.","volume":"10","author":"Sbardella","year":"2000","journal-title":"Med Chem Res"},{"key":"10.1016\/j.apsb.2019.08.009_bib32","doi-asserted-by":"crossref","first-page":"1778","DOI":"10.1021\/jm061167r","article-title":"Synthesis and anti-HIV-1 activity evaluation of 5-alkyl-2-alkylthio-6-(arylcarbonyl or \u03b1-cyanoarylmethyl)-3,4-dihydropyrimidin-4(3H)-ones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors","volume":"50","author":"Ji","year":"2007","journal-title":"J Med Chem"},{"key":"10.1016\/j.apsb.2019.08.009_bib33","doi-asserted-by":"crossref","first-page":"5212","DOI":"10.1021\/jm500284x","article-title":"Exploring the role of 2 chloro-6-fluoro substitution in 2-alkylthio-6-benzyl-5-alkylpyrimidin-4(3H)-ones: effects in HIV-1-infected cells and in HIV-1 reverse transcriptase enzymes","volume":"57","author":"Rotili","year":"2014","journal-title":"J Med Chem"},{"key":"10.1016\/j.apsb.2019.08.009_bib34","doi-asserted-by":"crossref","first-page":"2083","DOI":"10.1021\/acs.jmedchem.8b01729","volume":"62","author":"Huang","year":"2019","journal-title":"J Med Chem"},{"key":"10.1016\/j.apsb.2019.08.009_bib35","doi-asserted-by":"crossref","first-page":"212","DOI":"10.1016\/j.bioorg.2018.04.027","article-title":"Hit optimization studies of 3-hydroxy-indolin-2-one analogs as potential anti-HIV-1 agents","volume":"79","author":"Chander","year":"2018","journal-title":"Bioorg Chem"},{"key":"10.1016\/j.apsb.2019.08.009_bib36","article-title":"Azvudine, a novel nucleoside reverse transcriptase inhibitor showed good drug combination features and better inhibition on drug-resistant strains than lamivudine in\u00a0vitro","volume":"9","author":"Wang","year":"2014","journal-title":"PLoS One"},{"key":"10.1016\/j.apsb.2019.08.009_bib37","doi-asserted-by":"crossref","first-page":"257","DOI":"10.1016\/S0076-6879(96)75017-6","article-title":"Nonisotopic assays of viral polymerases and related proteins","volume":"275","author":"Eberle","year":"1996","journal-title":"Methods Enzymol"},{"key":"10.1016\/j.apsb.2019.08.009_bib38","doi-asserted-by":"crossref","first-page":"75","DOI":"10.1016\/j.bioorg.2016.05.009","article-title":"Rational design, synthesis, anti-HIV-1 RT and antimicrobial activity of novel 3-(6-methoxy-3,4-dihydroquinolin-1(2H)-yl)-1-(piperazin-1-yl)propan-1-one derivatives","volume":"67","author":"Chander","year":"2016","journal-title":"Bioorg Chem"},{"key":"10.1016\/j.apsb.2019.08.009_bib39","doi-asserted-by":"crossref","first-page":"1639","DOI":"10.1002\/(SICI)1096-987X(19981115)19:14<1639::AID-JCC10>3.0.CO;2-B","article-title":"Automated docking using a Lamarckian genetic algorithm and an empirical binding free energy function","volume":"19","author":"Morris","year":"1998","journal-title":"J Comput Chem"},{"key":"10.1016\/j.apsb.2019.08.009_bib40","doi-asserted-by":"crossref","first-page":"1145","DOI":"10.1002\/jcc.20634","article-title":"A semiempirical free energy force \ufb01eld with charge-based desolvation","volume":"28","author":"Huey","year":"2007","journal-title":"J Comput Chem"}],"container-title":["Acta Pharmaceutica Sinica B"],"original-title":[],"language":"en","link":[{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S2211383519303909?httpAccept=text\/xml","content-type":"text\/xml","content-version":"vor","intended-application":"text-mining"},{"URL":"https:\/\/api.elsevier.com\/content\/article\/PII:S2211383519303909?httpAccept=text\/plain","content-type":"text\/plain","content-version":"vor","intended-application":"text-mining"}],"deposited":{"date-parts":[[2025,10,31]],"date-time":"2025-10-31T16:44:00Z","timestamp":1761929040000},"score":1,"resource":{"primary":{"URL":"https:\/\/linkinghub.elsevier.com\/retrieve\/pii\/S2211383519303909"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2020,3]]},"references-count":40,"journal-issue":{"issue":"3","published-print":{"date-parts":[[2020,3]]}},"alternative-id":["S2211383519303909"],"URL":"https:\/\/doi.org\/10.1016\/j.apsb.2019.08.009","relation":{},"ISSN":["2211-3835"],"issn-type":[{"value":"2211-3835","type":"print"}],"subject":[],"published":{"date-parts":[[2020,3]]},"assertion":[{"value":"Elsevier","name":"publisher","label":"This article is maintained by"},{"value":"Synthesis and biological evaluation of a series of 2-(((5-akly\/aryl-1H-pyrazol-3-yl)methyl)thio)-5-alkyl-6-(cyclohexylmethyl)-pyrimidin-4(3H)-ones as potential HIV-1 inhibitors","name":"articletitle","label":"Article Title"},{"value":"Acta Pharmaceutica Sinica B","name":"journaltitle","label":"Journal Title"},{"value":"https:\/\/doi.org\/10.1016\/j.apsb.2019.08.009","name":"articlelink","label":"CrossRef DOI link to publisher maintained version"},{"value":"article","name":"content_type","label":"Content Type"},{"value":"\u00a9 2020 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier B.V.","name":"copyright","label":"Copyright"}]}}