Journal of medicinal chemistry

(J Med Chem) ISSNs: , 1520-4804

References in Journal of medicinal chemistry:

Title Authors Year
New Nitrogen Containing Substituents at the Indole-2-carboxamide Yield High Potent and Broad Spectrum Indolylarylsulfone HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors. La Regina G, Coluccia A, Brancale A, Piscitelli F, Famiglini V, Cosconati S, Maga G, Samuele A, Gonzales E, Clotet B, Schols D, Este J, Novellino E, Silvestri R 2012
Diarylpyrimidine-dihydrobenzyloxopyrimidine hybrids: new, wide-spectrum anti-HIV-1 agents active at (sub)-nanomolar level. Rotili D, Tarantino D, Artico M, Nawrozkij MB, Gonzalez-Ortega E, Clotet B, Samuele A, Esté JA, Maga G, Mai A 2011
Synthesis of novel diarylpyrimidine analogues and their antiviral activity against human immunodeficiency virus type 1. Guillemont J, Pasquier E, Palandjian P, Vernier D, Gaurrand S, Lewi PJ, Heeres J, De Jonge MR, Koymans LM, Daeyaert FF, Vinkers MH, Arnold E, Das K, Pauwels R, Andries K, De Béthune MP, Bettens E, Hertogs K, Wigerinck P, Timmerman P, Janssen PA 2005
Design, synthesis, and SAR of a novel pyrazinone series with non-nucleoside HIV-1 reverse transcriptase inhibitory activity. Heeres J, De Jonge MR, Koymans LM, Daeyaert FF, Vinkers MH, Van Aken KJ, Arnold E, Das K, Kilonda A, Hoornaert GJ, Compernolle F, Cegla M, Azzam RA, Andries K, De Béthune MP, Azijn H, Pauwels R, Lewi PJ, Janssen PA 2005
The nucleoside analogue D-carba T blocks HIV-1 reverse transcription. Boyer PL, Vu BC, Ambrose Z, Julias JG, Warnecke S, Liao C, Meier C, Marquez VE, Hughes SH 2009
A conformationally locked analogue of the anti-HIV agent stavudine. An important correlation between pseudorotation and maximum amplitude. Choi Y, George C, Comin MJ, Barchi JJ, Kim HS, Jacobson KA, Balzarini J, Mitsuya H, Boyer PL, Hughes SH, Marquez VE 2003
Potential anti-AIDS naphthalenesulfonic acid derivatives. Synthesis and inhibition of HIV-1 induced cytopathogenesis and HIV-1 and HIV-2 reverse transcriptase activities. Tan GT, Wickramasinghe A, Verma S, Singh R, Hughes SH, Pezzuto JM, Baba M, Mohan P 1992
Crystal structure of tert-butyldimethylsilyl-spiroaminooxathioledioxide-thymine (TSAO-T) in complex with HIV-1 reverse transcriptase (RT) redefines the elastic limits of the non-nucleoside inhibitor-binding pocket. Das K, Bauman JD, Rim AS, Dharia C, Clark AD, Camarasa MJ, Balzarini J, Arnold E 2011
4-Benzyl and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones: in vitro evaluation of new C-3-amino-substituted and C-5,6-alkyl-substituted analogues against clinically important HIV mutant strains. Benjahad A, Croisy M, Monneret C, Bisagni E, Mabire D, Coupa S, Poncelet A, Csoka I, Guillemont J, Meyer C, Andries K, Pauwels R, De Béthune MP, Himmel DM, Das K, Arnold E, Nguyen CH, Grierson DS 2005
Molecular modeling calculations of HIV-1 reverse transcriptase nonnucleoside inhibitors: correlation of binding energy with biological activity for novel 2-aryl-substituted benzimidazole analogues. Kroeger Smith MB, Hose BM, Hawkins A, Lipchock J, Farnsworth DW, Rizzo RC, Tirado-Rives J, Arnold E, Zhang W, Hughes SH, Jorgensen WL, Michejda CJ, Smith RH 2003
Synthesis and biological activity of novel nonnucleoside inhibitors of HIV-1 reverse transcriptase. 2-Aryl-substituted benzimidazoles. Roth T, Morningstar ML, Boyer PL, Hughes SH, Buckheit RW, Michejda CJ 1997
Synthesis, activity, and structural analysis of novel α-hydroxytropolone inhibitors of human immunodeficiency virus reverse transcriptase-associated ribonuclease H. Chung S, Himmel DM, Jiang JK, Wojtak K, Bauman JD, Rausch JW, Wilson JA, Beutler JA, Thomas CJ, Arnold E, Le Grice SF 2011
Conformational landscape of the human immunodeficiency virus type 1 reverse transcriptase non-nucleoside inhibitor binding pocket: lessons for inhibitor design from a cluster analysis of many crystal structures. Paris KA, Haq O, Felts AK, Das K, Arnold E, Levy RM 2009
Synthesis, biological activity, and crystal structure of potent nonnucleoside inhibitors of HIV-1 reverse transcriptase that retain activity against mutant forms of the enzyme. Morningstar ML, Roth T, Farnsworth DW, Smith MK, Watson KM, Buckheit RW, Das K, Zhang W, Arnold E, Julias JG, Hughes SH, Michejda CJ 2007
Design, synthesis, SAR, and molecular modeling studies of acylthiocarbamates: a novel series of potent non-nucleoside HIV-1 reverse transcriptase inhibitors structurally related to phenethylthiazolylthiourea derivatives. Ranise A, Spallarossa A, Schenone S, Bruno O, Bondavalli F, Vargiu L, Marceddu T, Mura M, La Colla P, Pani A 2003
New alkenyldiarylmethanes with enhanced potencies as anti-HIV agents which act as non-nucleoside reverse transcriptase inhibitors. Cushman M, Casimiro-Garcia A, Hejchman E, Ruell JA, Huang M, Schaeffer CA, Williamson K, Rice WG, Buckheit RW 1998
2-(Alkyl/Aryl)Amino-6-Benzylpyrimidin-4(3H)-ones as Inhibitors of Wild-Type and Mutant HIV-1: Enantioselectivity Studies. Rotili D, Samuele A, Tarantino D, Ragno R, Musmuca I, Ballante F, Botta G, Morera L, Pierini M, Cirilli R, Nawrozkij MB, Gonzalez E, Clotet B, Artico M, Esté JA, Maga G, Mai A 2012
Indolylarylsulfones bearing natural and unnatural amino acids. Discovery of potent inhibitors of HIV-1 non-nucleoside wild type and resistant mutant strains reverse transcriptase and coxsackie B4 virus. Piscitelli F, Coluccia A, Brancale A, La Regina G, Sansone A, Giordano C, Balzarini J, Maga G, Zanoli S, Samuele A, Cirilli R, La Torre F, Lavecchia A, Novellino E, Silvestri R 2009
Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. Design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity. Fattorusso C, Gemma S, Butini S, Huleatt P, Catalanotti B, Persico M, De Angelis M, Fiorini I, Nacci V, Ramunno A, Rodriquez M, Greco G, Novellino E, Bergamini A, Marini S, Coletta M, Maga G, Spadari S, Campiani G 2005
Quinoxalinylethylpyridylthioureas (QXPTs) as potent non-nucleoside HIV-1 reverse transcriptase (RT) inhibitors. Further SAR studies and identification of a novel orally bioavailable hydrazine-based antiviral agent. Campiani G, Aiello F, Fabbrini M, Morelli E, Ramunno A, Armaroli S, Nacci V, Garofalo A, Greco G, Novellino E, Maga G, Spadari S, Bergamini A, Ventura L, Bongiovanni B, Capozzi M, Bolacchi F, Marini S, Coletta M, Guiso G, Caccia S 2001
Pyrrolobenzoxazepinone derivatives as non-nucleoside HIV-1 RT inhibitors: further structure-activity relationship studies and identification of more potent broad-spectrum HIV-1 RT inhibitors with antiviral activity. Campiani G, Morelli E, Fabbrini M, Nacci V, Greco G, Novellino E, Ramunno A, Maga G, Spadari S, Caliendo G, Bergamini A, Faggioli E, Uccella I, Bolacchi F, Marini S, Coletta M, Nacca A, Caccia S 1999
Indolylarylsulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: new cyclic substituents at indole-2-carboxamide. La Regina G, Coluccia A, Brancale A, Piscitelli F, Gatti V, Maga G, Samuele A, Pannecouque C, Schols D, Balzarini J, Novellino E, Silvestri R 2011
Specific targeting of highly conserved residues in the HIV-1 reverse transcriptase primer grip region. 2. Stereoselective interaction to overcome the effects of drug resistant mutations. Butini S, Brindisi M, Cosconati S, Marinelli L, Borrelli G, Coccone SS, Ramunno A, Campiani G, Novellino E, Zanoli S, Samuele A, Giorgi G, Bergamini A, Di Mattia M, Lalli S, Galletti B, Gemma S, Maga G 2009
Discovery of chiral cyclopropyl dihydro-alkylthio-benzyl-oxopyrimidine (S-DABO) derivatives as potent HIV-1 reverse transcriptase inhibitors with high activity against clinically relevant mutants. Radi M, Maga G, Alongi M, Angeli L, Samuele A, Zanoli S, Bellucci L, Tafi A, Casaluce G, Giorgi G, Armand-Ugon M, Gonzalez E, Esté JA, Baltzinger M, Bec G, Dumas P, Ennifar E, Botta M 2009
Novel 1-[2-(diarylmethoxy)ethyl]-2-methyl-5-nitroimidazoles as HIV-1 non-nucleoside reverse transcriptase inhibitors. A structure-activity relationship investigation. De Martino G, La Regina G, Di Pasquali A, Ragno R, Bergamini A, Ciaprini C, Sinistro A, Maga G, Crespan E, Artico M, Silvestri R 2005
3-Hydroxypyrimidine-2,4-diones as an inhibitor scaffold of HIV integrase. Tang J, Maddali K, Metifiot M, Sham YY, Vince R, Pommier Y, Wang Z 2011
Indolyl aryl sulfones as HIV-1 non-nucleoside reverse transcriptase inhibitors: role of two halogen atoms at the indole ring in developing new analogues with improved antiviral activity. Regina GL, Coluccia A, Piscitelli F, Bergamini A, Sinistro A, Cavazza A, Maga G, Samuele A, Zanoli S, Novellino E, Artico M, Silvestri R 2007
Rationally designed dual inhibitors of HIV reverse transcriptase and integrase. Wang Z, Bennett EM, Wilson DJ, Salomon CE, Vince R 2007
D- and L-2',3'-didehydro-2',3'-dideoxy-3'-fluoro-carbocyclic nucleosides: synthesis, anti-HIV activity and mechanism of resistance. Wang J, Jin Y, Rapp KL, Schinazi RF, Chu CK 2007
Hierarchical database screenings for HIV-1 reverse transcriptase using a pharmacophore model, rigid docking, solvation docking, and MM-PB/SA. Wang J, Kang X, Kuntz ID, Kollman PA 2005
Activation of human telomerase reverse transcriptase expression by some new symmetrical bis-substituted derivatives of the anthraquinone. Huang HS, Chiou JF, Fong Y, Hou CC, Lu YC, Wang JY, Shih JW, Pan YR, Lin JJ 2003
Newly synthesized L-enantiomers of 3'-fluoro-modified beta-2'-deoxyribonucleoside 5'-triphosphates inhibit hepatitis B DNA polymerases but not the five cellular DNA polymerases alpha, beta, gamma, delta, and epsilon nor HIV-1 reverse transcriptase. von Janta-Lipinski M, Costisella B, Ochs H, Hübscher U, Hafkemeyer P, Matthes E 1998
The application of phosphoramidate protide technology to acyclovir confers anti-HIV inhibition. Derudas M, Carta D, Brancale A, Vanpouille C, Lisco A, Margolis L, Balzarini J, McGuigan C 2009
Betulinic acid derivatives: a new class of human immunodeficiency virus type 1 specific inhibitors with a new mode of action. Evers M, Poujade C, Soler F, Ribeill Y, James C, Lelièvre Y, Gueguen JC, Reisdorf D, Morize I, Pauwels R, De Clercq E, Hénin Y, Bousseau A, Mayaux JF, Le Pecq JB, Dereu N 1996
Deoxyribonucleoside 2'- or 3'-mixed disulfides: prodrugs to target ribonucleotide reductase and/or to inhibit HIV reverse transcription. Roy B, Chambert S, Lepoivre M, Aubertin AM, Balzarini J, Décout JL 2003
Synthesis, anti-HIV activity, and metabolic stability of new alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors. Deng BL, Hartman TL, Buckheit RW, Pannecouque C, De Clercq E, Fanwick PE, Cushman M 2005
Strategies for the design of HIV-1 non-nucleoside reverse transcriptase inhibitors: lessons from the development of seven representative paradigms. Li D, Zhan P, De Clercq E, Liu X 2012
First synthesis and evaluation of the inhibitory effects of aza analogues of TSAO on HIV-1 replication. Nguyen Van Nhien A, Tomassi C, Len C, Marco-Contelles JL, Balzarini J, Pannecouque C, De Clercq E, Postel D 2005
Synthesis and anti-HIV activity of new metabolically stable alkenyldiarylmethane non-nucleoside reverse transcriptase inhibitors incorporating N-methoxy imidoyl halide and 1,2,4-oxadiazole systems. Sakamoto T, Cullen MD, Hartman TL, Watson KM, Buckheit RW, Pannecouque C, De Clercq E, Cushman M 2007
3'-C-branched 2'-deoxy-5-methyluridines: synthesis, enzyme inhibition, and antiviral properties. Fedorov II, Kazmina EM, Novicov NA, Gurskaya GV, Bochkarev AV, Jasko MV, Victorova LS, Kukhanova MK, Balzarini J, De Clercq E 1992
Synthesis of 3' '-substituted TSAO derivatives with anti-HIV-1 and anti-HIV-2 activity through an efficient palladium-catalyzed cross-coupling approach. Lobatón E, Rodríguez-Barrios F, Gago F, Pérez-Pérez MJ, De Clercq E, Balzarini J, Camarasa MJ, Velázquez S 2002
Potential multifunctional inhibitors of HIV-1 reverse transcriptase. Novel [AZT]-[TSAO-T] and [d4T]-[TSAO-T] heterodimers modified in the linker and in the dideoxynucleoside region. Velázquez S, Tuñón V, Jimeno ML, Chamorro C, De Clercq E, Balzarini J, Camarasa MJ 1999
The synthesis of nucleoside 5'-O-(1,1-dithiotriphosphates). Okruszek A, Olesiak M, Balzarini J 1994
N-aminoimidazole derivatives inhibiting retroviral replication via a yet unidentified mode of action. Lagoja IM, Pannecouque C, Van Aerschot A, Witvrouw M, Debyser Z, Balzarini J, Herdewijn P, De Clercq E 2003
Synthesis and anti-HIV-1 activity evaluation of 5-alkyl-2-alkylthio-6-(arylcarbonyl or alpha-cyanoarylmethyl)-3,4-dihydropyrimidin-4(3H)-ones as novel non-nucleoside HIV-1 reverse transcriptase inhibitors. Ji L, Chen FE, De Clercq E, Balzarini J, Pannecouque C 2007
4"-Benzoylureido-TSAO derivatives as potent and selective non-nucleoside HCMV inhibitors. Structure-activity relationship and mechanism of antiviral action. de Castro S, Peromingo MT, Naesens L, Andrei G, Snoeck R, Balzarini J, Velázquez S, Camarasa MJ 2008
Novel antiviral C5-substituted pyrimidine acyclic nucleoside phosphonates selected as human thymidylate kinase substrates. Topalis D, Pradère U, Roy V, Caillat C, Azzouzi A, Broggi J, Snoeck R, Andrei G, Lin J, Eriksson S, Alexandre JA, El-Amri C, Deville-Bonne D, Meyer P, Balzarini J, Agrofoglio LA 2011
Structure-activity relationships of [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]- 3'-spiro-5' '-(4' '-amino-1' ',2' '-oxathiole-2' ',2' '-dioxide)thymine derivatives as inhibitors of HIV-1 reverse transcriptase dimerization. Sluis-Cremer N, Hamamouch N, San Félix A, Velazquez S, Balzarini J, Camarasa MJ 2006
Novel 1,1,3-trioxo-2H,4H-thieno[3,4-e][1,2,4]thiadiazine derivatives as non-nucleoside reverse transcriptase inhibitors that inhibit human immunodeficiency virus type 1 replication. Arranz E, Díaz JA, Ingate ST, Witvrouw M, Pannecouque C, Balzarini J, De Clercq E, Vega S 1998
Identification of a putative binding site for [2',5'-bis-O-(tert-butyldimethylsilyl)-beta-D-ribofuranosyl]-3'-spiro-5''-(4''-amino-1'',2''-oxathiole-2'',2''-dioxide)thymine (TSAO) derivatives at the p51-p66 interface of HIV-1 reverse transcriptase. Rodríguez-Barrios F, Pérez C, Lobatón E, Velázquez S, Chamorro C, San-Félix A, Pérez-Pérez MJ, Camarasa MJ, Pelemans H, Balzarini J, Gago F 2001
Abasic analogues of TSAO-T as the first sugar derivatives that specifically inhibit HIV-1 reverse transcriptase. Velázquez S, Chamorro C, Pérez-Pérez MJ, Alvarez R, Jimeno ML, Martín-Domenech A, Pérez C, Gago F, De Clercq E, Balzarini J, San-Félix A, Camarasa MJ 1998
Synthesis and anti-HIV activity of [AZT]-[TSAO-T] and [AZT]-[HEPT] dimers as potential multifunctional inhibitors of HIV-1 reverse transcriptase. Velázquez S, Alvarez R, San-Félix A, Jimeno ML, De Clercq E, Balzarini J, Camarasa MJ 1995
Replacement of the metabolically labile methyl esters in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors with isoxazolone, isoxazole, oxazolone, or cyano substituents. Deng BL, Hartman TL, Buckheit RW, Pannecouque C, De Clercq E, Cushman M 2006
Design, synthesis, anti-HIV activities, and metabolic stabilities of alkenyldiarylmethane (ADAM) non-nucleoside reverse transcriptase inhibitors. Silvestri MA, Nagarajan M, De Clercq E, Pannecouque C, Cushman M 2004
Preparation and anti-HIV activities of aurintricarboxylic acid fractions and analogues: direct correlation of antiviral potency with molecular weight. Cushman M, Wang PL, Chang SH, Wild C, De Clercq E, Schols D, Goldman ME, Bowen JA 1991
Betulinic acid derivatives: a new class of specific inhibitors of human immunodeficiency virus type 1 entry. Soler F, Poujade C, Evers M, Carry JC, Hénin Y, Bousseau A, Huet T, Pauwels R, De Clercq E, Mayaux JF, Le Pecq JB, Dereu N 1996
Synthesis and anti-HIV activities of low molecular weight aurintricarboxylic acid fragments and related compounds. Cushman M, Kanamathareddy S, De Clercq E, Schols D, Goldman ME, Bowen JA 1991
Gliotoxin analogues as inhibitors of reverse transcriptase. 2. Resolution and X-ray crystal structure determination. Ottenheijm HC, Herscheid JD, Tijhuis MW, Nivard RJ, De Clercq E, Prick PA 1978
Gliotoxin analogues as inhibitors of reverse transcriptase. 1. Effect of lipophilicity. Ottenheijm HC, Herscheid JD, Tijhuis MW, Oosterbaan M, De Clercq E 1978
Synthesis and biological evaluation of alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors that possess increased hydrolytic stability. Cullen MD, Deng BL, Hartman TL, Watson KM, Buckheit RW, Pannecouque C, Clercq ED, Cushman M 2007
Detecting allosteric sites of HIV-1 reverse transcriptase by X-ray crystallographic fragment screening. Bauman JD, Patel D, Dharia C, Fromer M, Ahmed S, Frenkel YV, Eck JT, Ho WC, Das K, Shatkin AJ, Arnold E 2013
Clicking 3'-azidothymidine into novel potent inhibitors of human immunodeficiency virus. Sirivolu VR, Verneka SK, Ilina T, Myshakina NS, Parniak MA, Wang Z 2013
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