436
mapping has allowed us to think of novel targets at fusion, maturation, and capsid
assembly stage. These new targets need to be followed with dedicated discovery programs to bring new drugs to the market.
References
Ali A, Reddy GSK, Nalam MNL, Anjum SG, Cao H, Schiffer CA, Rana TM (2010) Structurebased design, synthesis, and structure activity relationship studies of HIV-1 protease inhibitors
incorporating phenyloxazolidinones. J Med Chem 53(21):7699–7708
Athanassiou Z, Dias RLA, Moehle K, Dobson N, Varani G, Robinson JA (2004) Structural mimicry of retroviral tat proteins by constrained beta-hairpin peptidomimetics: ligands with high
affinity and selectivity for viral TAR RNA regulatory elements. J Am Chem Soc
126(22):6906–6913
Athanassiou Z, Patora K, Dias RLA, Moehle K, Robinson JA, Varani G (2007) Structure-guided
peptidomimetic design leads to nanomolar beta-hairpin inhibitors of the Tat-TAR interaction of
bovine immunodeficiency virus. Biochemistry 46(3):741–751
Billamboz M, Suchaud V, Bailly F, Lion C, Andréola M, Christ F, Debyser Z, Cotelle P (2016)
2-hydroxyisoquinoline-1,3(2H,4H)-diones (HIDs) as human immunodeficiency virus type 1
integrase inhibitors: influence of the alkylcarboxamide substitution of position 4. Eur J Med
Chem 117:256–268
Bungard CJ, Williams PD, Ballard JE, Bennett DJ, Beaulieu C, Bahnck-Teets C, Carroll SS,
Chang RK, Dubost DC, Fay JF, Diamond TL, Greshock TJ, Hao L, Holloway MK, Felock PJ,
Gesell JJ, Su HP, Manikowski JJ, McKay DJ, Miller M, Min X, Molinaro C, Moradei OM,
Nantermet PG, Nadeau C, Sanchez RI, Satyanarayana T, Shipe WD, Singh SK, Truong VL,
Vijayasaradhi S, Wiscount CM, Vacca JP, Crane SN, McCauley JA (2016) Discovery of
MK-8718, an HIV protease inhibitor containing a novel morpholine aspartate binding group.
ACS Med Chem Lett 7(7):702–707
Chong P, Sebahar P, Youngman M, Garrido D, Zhang H, Stewart EL, Nolte RT, Wang L, Ferris RG,
Edelstein M, Weaver K, Mathis A, Peat A (2012) Rational design of potent non-nucleoside
inhibitors of HIV-1 reverse transcriptase. J Med Chem 55(23):10601–10609
Dassonneville L, Hamy F, Colson P, Houssier C, Bailly C (1997) Binding of hoechst 33258 to the
TAR RNA of HIV-1. Recognition of a pyrimidine bulge-dependent structure. Nucleic Acids
Res 25(22):4487–4492
Dogo-Isonagie C, Lee S, Lohith K, Liu H, Mandadapu S. R, Lusvarghi S, O’Connor RD, Bewley
CA (2016) Design and synthesis of small molecule-sulfotyrosine mimetics that inhibit HIV-1
entry. Bioorg Med Chem 24(8): 1718–1728.
Dong M, Lu L, Li H, Wang X, Lu H, Jiang S, Dai QY (2012) Design, synthesis, and biological
activity of novel 1,4-disubstituted piperidine/piperazine derivatives as CCR5 antagonist-based
HIV-1 entry inhibitors. Bioorg Med Chem Lett 22(9):3284–3286
Ganguly AK, Alluri SS, Wang C, Antropow A, White A, Caroccia D, Biswas D, Kang E, Zhang
LK, Carroll SS, Burlein C, Fay J, Orth P, Strickland C (2014) Structural optimization of cyclic
sulfonamide based novel HIV-1 protease inhibitors to picomolar affinities guided by X-ray
crystallographic analysis. Tetrahedron 70(18):2894–2904
Gao B, Zhang C, Yin Y, Tang L, Liu Z (2011) Design and synthesis of potent HIV-1 protease
inhibitors incorporating hydroxyprolinamides as novel P2 ligands. Bioorg Med Chem Lett
21(12):3730–3733
Ghosh AK, Osswald HL, Prato G (2016) Recent progress in the development of HIV-1 protease
inhibitors for the treatment of HIV/AIDS. J Med Chem 59(11):5172–5208
Gu W, Ip DT, Liu S, Chan JH, Wang Y, Zhang X, Zheng YT, Wan DC (2014) 1,4-bis(5-(naphthalen1- yl) thiophen-2-yl)naphthalene, a small molecule, functions as a novel anti-HIV-1 inhibitor
targeting the interaction between integrase and cellular lens epithelium-derived growth factor.
Chem Biol Interact 213:21–27
N. Ranjan et al.
mapping has allowed us to think of novel targets at fusion, maturation, and capsid
assembly stage. These new targets need to be followed with dedicated discovery programs to bring new drugs to the market.
References
Ali A, Reddy GSK, Nalam MNL, Anjum SG, Cao H, Schiffer CA, Rana TM (2010) Structurebased design, synthesis, and structure activity relationship studies of HIV-1 protease inhibitors
incorporating phenyloxazolidinones. J Med Chem 53(21):7699–7708
Athanassiou Z, Dias RLA, Moehle K, Dobson N, Varani G, Robinson JA (2004) Structural mimicry of retroviral tat proteins by constrained beta-hairpin peptidomimetics: ligands with high
affinity and selectivity for viral TAR RNA regulatory elements. J Am Chem Soc
126(22):6906–6913
Athanassiou Z, Patora K, Dias RLA, Moehle K, Robinson JA, Varani G (2007) Structure-guided
peptidomimetic design leads to nanomolar beta-hairpin inhibitors of the Tat-TAR interaction of
bovine immunodeficiency virus. Biochemistry 46(3):741–751
Billamboz M, Suchaud V, Bailly F, Lion C, Andréola M, Christ F, Debyser Z, Cotelle P (2016)
2-hydroxyisoquinoline-1,3(2H,4H)-diones (HIDs) as human immunodeficiency virus type 1
integrase inhibitors: influence of the alkylcarboxamide substitution of position 4. Eur J Med
Chem 117:256–268
Bungard CJ, Williams PD, Ballard JE, Bennett DJ, Beaulieu C, Bahnck-Teets C, Carroll SS,
Chang RK, Dubost DC, Fay JF, Diamond TL, Greshock TJ, Hao L, Holloway MK, Felock PJ,
Gesell JJ, Su HP, Manikowski JJ, McKay DJ, Miller M, Min X, Molinaro C, Moradei OM,
Nantermet PG, Nadeau C, Sanchez RI, Satyanarayana T, Shipe WD, Singh SK, Truong VL,
Vijayasaradhi S, Wiscount CM, Vacca JP, Crane SN, McCauley JA (2016) Discovery of
MK-8718, an HIV protease inhibitor containing a novel morpholine aspartate binding group.
ACS Med Chem Lett 7(7):702–707
Chong P, Sebahar P, Youngman M, Garrido D, Zhang H, Stewart EL, Nolte RT, Wang L, Ferris RG,
Edelstein M, Weaver K, Mathis A, Peat A (2012) Rational design of potent non-nucleoside
inhibitors of HIV-1 reverse transcriptase. J Med Chem 55(23):10601–10609
Dassonneville L, Hamy F, Colson P, Houssier C, Bailly C (1997) Binding of hoechst 33258 to the
TAR RNA of HIV-1. Recognition of a pyrimidine bulge-dependent structure. Nucleic Acids
Res 25(22):4487–4492
Dogo-Isonagie C, Lee S, Lohith K, Liu H, Mandadapu S. R, Lusvarghi S, O’Connor RD, Bewley
CA (2016) Design and synthesis of small molecule-sulfotyrosine mimetics that inhibit HIV-1
entry. Bioorg Med Chem 24(8): 1718–1728.
Dong M, Lu L, Li H, Wang X, Lu H, Jiang S, Dai QY (2012) Design, synthesis, and biological
activity of novel 1,4-disubstituted piperidine/piperazine derivatives as CCR5 antagonist-based
HIV-1 entry inhibitors. Bioorg Med Chem Lett 22(9):3284–3286
Ganguly AK, Alluri SS, Wang C, Antropow A, White A, Caroccia D, Biswas D, Kang E, Zhang
LK, Carroll SS, Burlein C, Fay J, Orth P, Strickland C (2014) Structural optimization of cyclic
sulfonamide based novel HIV-1 protease inhibitors to picomolar affinities guided by X-ray
crystallographic analysis. Tetrahedron 70(18):2894–2904
Gao B, Zhang C, Yin Y, Tang L, Liu Z (2011) Design and synthesis of potent HIV-1 protease
inhibitors incorporating hydroxyprolinamides as novel P2 ligands. Bioorg Med Chem Lett
21(12):3730–3733
Ghosh AK, Osswald HL, Prato G (2016) Recent progress in the development of HIV-1 protease
inhibitors for the treatment of HIV/AIDS. J Med Chem 59(11):5172–5208
Gu W, Ip DT, Liu S, Chan JH, Wang Y, Zhang X, Zheng YT, Wan DC (2014) 1,4-bis(5-(naphthalen1- yl) thiophen-2-yl)naphthalene, a small molecule, functions as a novel anti-HIV-1 inhibitor
targeting the interaction between integrase and cellular lens epithelium-derived growth factor.
Chem Biol Interact 213:21–27
N. Ranjan et al.