437
Hughes JP, Rees S, Kalindjian SB, Philpott KL (2010) Principles of early drug discovery. Br
J Pharmacol 162(6):1239–1249
Kankanala J, Kirby KA, Liu F, Miller L, Nagy E, Wilson DJ, Parniak MA, Sarafianos SG, Wang Z
(2016) Design, synthesis, and biological evaluations of hydroxypyridonecarboxylic acids as
inhibitors of HIV reverse transcriptase associated RNase H. J Med Chem 59(10):5051–5062
Kim J, Lee D, Park C, So W, Jo M, Ok T, Kwon J, Kong S, Jo S, Kim Y, Choi J, Kim HC, Ko Y,
Choi I, Park Y, Yoon J, Ju MK, Kim J, Han SJ, Kim TH, Cechetto J, Nam J, Sommer P, Liuzzi
M, Lee J, No Z (2012) Discovery of phenylaminopyridine derivatives as novel HIV-1 nonnucleoside reverse transcriptase inhibitors. ACS Med Chem Lett 3(8):678–682
Kumar S, Kellish P, Robinson WE, Wang D, Appella DH, Arya DP (2012) Click dimers to target
HIV TAR RNA conformation. Biochemistry 51:2331–2347
Kumar S, Ranjan N, Kellish P, Gong C, Watkins D, Arya DP (2016) Multivalency in the recognition and antagonism of a HIV TAR RNA-TAT assembly using an aminoglycoside benzimidazole scaffold. Org Biomol Chem 14(6):2052–2056
Liu Z, Swidorski JJ, Nowicka-Sans B, Terry B, Protack T, Lin Z, Samanta H, Zhang S, Li Z, Parker
DD, Rahematpura S, Jenkins S, Beno BR, Krystal M, Meanwell NA, Dicker IB, Regueiro-Ren
A (2016) C-3 benzoic acid derivatives of C-3 deoxybetulinic acid and deoxybetulin as HIV-1
maturation inhibitors. Bioorg Med Chem 24(8):1757–1770
Luedtke NW, Tor Y (2003) Fluorescence-based methods for evaluating the RNA affinity and specificity of HIV-1 rev? RRE inhibitors. Biopolymers 70(1):103–119
Macarron R (2006) Critical review of the role of HTS in drug discovery. Drug Discov Today
11(7):277–279
Mayr LM, Bojanic D (2009) Novel trends in high-throughput screening. Curr Opin Pharmacol;
Anti-infect/New Technol 9(5):580–588
Mizuguchi T, Harada S, Miura T, Ohashi N, Narumi T, Mori H, Irahara Y, Yamada Y, Nomura W,
Matsushita S, Yoshimura K, Tamamura H (2016) A minimally cytotoxic CD4 mimic as an HIV
entry inhibitor. Bioorg Med Chem Lett 26(2):397–400
Munos B (2009) Lessons from 60 years of pharmaceutical innovation. Nat Rev Drug Discov
8(12):959–968
O’Hara BM, Olson WC (2002) HIV entry inhibitors in clinical development. Curr Opin Pharmacol
2(5):523–528
Ohrngren P, Wu X, Persson M, Ekegren JK, Wallberg H, Vrang L, Rosenquist A, Samuelsson B,
Unge T, Larhed M (2011) HIV-1 protease inhibitors with a tertiary alcohol containing
transition- state mimic and various P2 and P1prime or minute substituents. Med Chem Commun
2(8):701–709
Patel RV, Park SW (2015) Pyrroloaryls and pyrroloheteroaryls: inhibitors of the HIV fusion/attachment, reverse transcriptase and integrase. Bioorg Med Chem 23(17):5247–5263
Paul SM, Mytelka DS, Dunwiddie CT, Persinger CC, Munos BH, Lindborg SR, Schacht AL
(2010) How to improve R&D productivity: the pharmaceutical industry’s grand challenge. Nat
Rev Drug Discov 9(3):203–214
Peytou V, Condom R, Patino N, Guedj R, Aubertin A, Gelus N, Bailly C, Terreux R, Cabrol-Bass
D (1999) Synthesis and antiviral activity of ethidium-arginine conjugates directed against the
TAR RNA of HIV-1. J Med Chem 42(20):4042–4053
Qiu X, Zhao G, Tang L, Liu Z (2014) Design and synthesis of highly potent HIV-1 protease inhibitors with novel isosorbide-derived P2 ligands. Bioorg Med Chem Lett 24(11):2465–2468
Ramana LN, Anand AR, Sethuraman S, Krishnan UM (2014) Targeting strategies for delivery of
anti-HIV drugs. J Control Release 192:271–283
Ranjan N, Kumar S, Watkins D, Wang D, Appella DH, Arya DP (2013) Recognition of HIV-TAR
RNA using neomycin–benzimidazole conjugates. Bioorg Med Chem Lett 23(20):5689–5693
Swidorski JJ, Liu Z, Yin Z, Wang T, Carini DJ, Rahematpura S, Zheng M, Johnson K, Zhang S,
Lin PF, Parker DD, Li W, Meanwell NA, Hamann LG, Regueiro-Ren A (2016) Inhibitors of
HIV-1 attachment: the discovery and structure–activity relationships of tetrahydroisoquinolines
as replacements for the piperazine benzamide in the 3-glyoxylyl 6-azaindole pharmacophore.
Bioorg Med Chem Lett 26(1):160–167
18 Novel Targets and Advancements in Drug Discovery: The Case of HIV-AIDS
Hughes JP, Rees S, Kalindjian SB, Philpott KL (2010) Principles of early drug discovery. Br
J Pharmacol 162(6):1239–1249
Kankanala J, Kirby KA, Liu F, Miller L, Nagy E, Wilson DJ, Parniak MA, Sarafianos SG, Wang Z
(2016) Design, synthesis, and biological evaluations of hydroxypyridonecarboxylic acids as
inhibitors of HIV reverse transcriptase associated RNase H. J Med Chem 59(10):5051–5062
Kim J, Lee D, Park C, So W, Jo M, Ok T, Kwon J, Kong S, Jo S, Kim Y, Choi J, Kim HC, Ko Y,
Choi I, Park Y, Yoon J, Ju MK, Kim J, Han SJ, Kim TH, Cechetto J, Nam J, Sommer P, Liuzzi
M, Lee J, No Z (2012) Discovery of phenylaminopyridine derivatives as novel HIV-1 nonnucleoside reverse transcriptase inhibitors. ACS Med Chem Lett 3(8):678–682
Kumar S, Kellish P, Robinson WE, Wang D, Appella DH, Arya DP (2012) Click dimers to target
HIV TAR RNA conformation. Biochemistry 51:2331–2347
Kumar S, Ranjan N, Kellish P, Gong C, Watkins D, Arya DP (2016) Multivalency in the recognition and antagonism of a HIV TAR RNA-TAT assembly using an aminoglycoside benzimidazole scaffold. Org Biomol Chem 14(6):2052–2056
Liu Z, Swidorski JJ, Nowicka-Sans B, Terry B, Protack T, Lin Z, Samanta H, Zhang S, Li Z, Parker
DD, Rahematpura S, Jenkins S, Beno BR, Krystal M, Meanwell NA, Dicker IB, Regueiro-Ren
A (2016) C-3 benzoic acid derivatives of C-3 deoxybetulinic acid and deoxybetulin as HIV-1
maturation inhibitors. Bioorg Med Chem 24(8):1757–1770
Luedtke NW, Tor Y (2003) Fluorescence-based methods for evaluating the RNA affinity and specificity of HIV-1 rev? RRE inhibitors. Biopolymers 70(1):103–119
Macarron R (2006) Critical review of the role of HTS in drug discovery. Drug Discov Today
11(7):277–279
Mayr LM, Bojanic D (2009) Novel trends in high-throughput screening. Curr Opin Pharmacol;
Anti-infect/New Technol 9(5):580–588
Mizuguchi T, Harada S, Miura T, Ohashi N, Narumi T, Mori H, Irahara Y, Yamada Y, Nomura W,
Matsushita S, Yoshimura K, Tamamura H (2016) A minimally cytotoxic CD4 mimic as an HIV
entry inhibitor. Bioorg Med Chem Lett 26(2):397–400
Munos B (2009) Lessons from 60 years of pharmaceutical innovation. Nat Rev Drug Discov
8(12):959–968
O’Hara BM, Olson WC (2002) HIV entry inhibitors in clinical development. Curr Opin Pharmacol
2(5):523–528
Ohrngren P, Wu X, Persson M, Ekegren JK, Wallberg H, Vrang L, Rosenquist A, Samuelsson B,
Unge T, Larhed M (2011) HIV-1 protease inhibitors with a tertiary alcohol containing
transition- state mimic and various P2 and P1prime or minute substituents. Med Chem Commun
2(8):701–709
Patel RV, Park SW (2015) Pyrroloaryls and pyrroloheteroaryls: inhibitors of the HIV fusion/attachment, reverse transcriptase and integrase. Bioorg Med Chem 23(17):5247–5263
Paul SM, Mytelka DS, Dunwiddie CT, Persinger CC, Munos BH, Lindborg SR, Schacht AL
(2010) How to improve R&D productivity: the pharmaceutical industry’s grand challenge. Nat
Rev Drug Discov 9(3):203–214
Peytou V, Condom R, Patino N, Guedj R, Aubertin A, Gelus N, Bailly C, Terreux R, Cabrol-Bass
D (1999) Synthesis and antiviral activity of ethidium-arginine conjugates directed against the
TAR RNA of HIV-1. J Med Chem 42(20):4042–4053
Qiu X, Zhao G, Tang L, Liu Z (2014) Design and synthesis of highly potent HIV-1 protease inhibitors with novel isosorbide-derived P2 ligands. Bioorg Med Chem Lett 24(11):2465–2468
Ramana LN, Anand AR, Sethuraman S, Krishnan UM (2014) Targeting strategies for delivery of
anti-HIV drugs. J Control Release 192:271–283
Ranjan N, Kumar S, Watkins D, Wang D, Appella DH, Arya DP (2013) Recognition of HIV-TAR
RNA using neomycin–benzimidazole conjugates. Bioorg Med Chem Lett 23(20):5689–5693
Swidorski JJ, Liu Z, Yin Z, Wang T, Carini DJ, Rahematpura S, Zheng M, Johnson K, Zhang S,
Lin PF, Parker DD, Li W, Meanwell NA, Hamann LG, Regueiro-Ren A (2016) Inhibitors of
HIV-1 attachment: the discovery and structure–activity relationships of tetrahydroisoquinolines
as replacements for the piperazine benzamide in the 3-glyoxylyl 6-azaindole pharmacophore.
Bioorg Med Chem Lett 26(1):160–167
18 Novel Targets and Advancements in Drug Discovery: The Case of HIV-AIDS