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Volumn 5, Issue 4, 2002, Pages 594-605

Solid-phase compound library synthesis in drug design and development

Author keywords

Compound library; Drug discovery; Lead optimization; Parallel synthesis; Solid phase organic synthesis

Indexed keywords

INDOLE DERIVATIVE;

EID: 0036652153     PISSN: 13676733     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review
Times cited : (15)

References (21)
  • 1
    • 0035513630 scopus 로고    scopus 로고
    • Comprehensive survey of combinatorial library synthesis: 2000
    • Dolle RE: Comprehensive survey of combinatorial library synthesis: 2000. J Combinatorial Chem (2001) 3:477-517.
    • (2001) J Combinatorial Chem , vol.3 , pp. 477-517
    • Dolle, R.E.1
  • 3
    • 0034684780 scopus 로고    scopus 로고
    • 2A antagonist
    • 2A antagonist. Bioorg Med Chem Lett (2000) 10:2693-2696. This paper illustrates the use of organometallic chemistry in the construction of a library of pharmacologically relevant compounds, which in turn has yielded novel, potent and selective lead material at a GPCR.
    • (2000) Bioorg Med Chem Lett , vol.10 , pp. 2693-2696
    • Smith, A.L.1    Stevenson, G.I.2    Lewis, S.3    Patel, S.4    Castro, J.L.5
  • 4
    • 18244382828 scopus 로고    scopus 로고
    • Combinatorial synthesis of 3-(amidoalkyl) and 3-(aminoalkyl)-2-arylindole derivatives: Discovery of potent ligands for a variety of G-protein coupled receptors
    • Willoughby CA, Hutchins SM, Rosauer KG, Dhar MJ, Chapman KT, Chicchi GG, Sadowski S, Weinberg DH, Patel S, Malkowitz L, Di Salvo J, Pacholok SG, Cheng K: Combinatorial synthesis of 3-(amidoalkyl) and 3-(aminoalkyl)-2-arylindole derivatives: Discovery of potent ligands for a variety of G-protein coupled receptors. Bioorg Med Chem Lett (2002) 12:93-96. An interesting example of how library design based upon pharmacologically well-precedented structures can provide a rich variety of leads within a receptor superfamily. This paper also demonstrates the use of synthesis in mixtures in order to rapidly prepare large numbers of analogs.
    • (2002) Bioorg Med Chem Lett , vol.12 , pp. 93-96
    • Willoughby, C.A.1    Hutchins, S.M.2    Rosauer, K.G.3    Dhar, M.J.4    Chapman, K.T.5    Chicchi, G.G.6    Sadowski, S.7    Weinberg, D.H.8    Patel, S.9    Malkowitz, L.10    Di Salvo, J.11    Pacholok, S.G.12    Cheng, K.13
  • 7
    • 0035931355 scopus 로고    scopus 로고
    • Solid-phase synthesis of cyclic alkoxyketones, inhibitors of the cysteine protease cathepsin K
    • Fenwick AE, Garnier B, Gribble AD, Ife RJ, Rawlings AD, Witherington J: Solid-phase synthesis of cyclic alkoxyketones, inhibitors of the cysteine protease cathepsin K. Bioorg Med Chem Lett (2001) 11:195-198. An example of the use of IRORI technology to allow discrete, single compounds to be synthesised using the efficient 'mix-and-split' solid-phase synthesis technique.
    • (2001) Bioorg Med Chem Lett , vol.11 , pp. 195-198
    • Fenwick, A.E.1    Garnier, B.2    Gribble, A.D.3    Ife, R.J.4    Rawlings, A.D.5    Witherington, J.6
  • 8
    • 0035921097 scopus 로고    scopus 로고
    • Amino acid derived sulphonamide hydroxamates as inhibitors of procollagen C-proteinase: Solid-phase synthesis of ornithine analogues
    • Dankwart SM, Martin RL, Chan CS, Van Wart HE, Walker KAM, Delaet NG, Robinson LA: Amino acid derived sulphonamide hydroxamates as inhibitors of procollagen C-proteinase: Solid-phase synthesis of ornithine analogues. Bioorg Med Chem Lett (2001) 11:2085-2088.
    • (2001) Bioorg Med Chem Lett , vol.11 , pp. 2085-2088
    • Dankwart, S.M.1    Martin, R.L.2    Chan, C.S.3    Van Wart, H.E.4    Walker, K.A.M.5    Delaet, N.G.6    Robinson, L.A.7
  • 10
    • 0035931468 scopus 로고    scopus 로고
    • Solid-phase optimisation of achiral amidinobenzyl indoles as potent and selective factor Xa inhibitors
    • Heinelt U, Herok S, Matter H, Wildgoose P: Solid-phase optimisation of achiral amidinobenzyl indoles as potent and selective factor Xa inhibitors. Bioorg Med Chem Lett (2001) 11:227-230. This paper provides an interesting example of the solid-phase synthesis to rapidly optimize the pharmacokinetic profile of an existing lead.
    • (2001) Bioorg Med Chem Lett , vol.11 , pp. 227-230
    • Heinelt, U.1    Herok, S.2    Matter, H.3    Wildgoose, P.4
  • 12
    • 0035829149 scopus 로고    scopus 로고
    • Solid-phase synthesis of a library constructed of aromatic phosphate, long alkyl chains and tryptophane components, and identification of potent dipeptide telomerase inhibitors
    • Sasaki S, Ehara T, Alam MR, Fujino Y, Harada N, Kimura J, Nakamura H, Maeda M: Solid-phase synthesis of a library constructed of aromatic phosphate, long alkyl chains and tryptophane components, and identification of potent dipeptide telomerase inhibitors. Bioorg Med Chem Lett (2001) 11:2581-2584.
    • (2001) Bioorg Med Chem Lett , vol.11 , pp. 2581-2584
    • Sasaki, S.1    Ehara, T.2    Alam, M.R.3    Fujino, Y.4    Harada, N.5    Kimura, J.6    Nakamura, H.7    Maeda, M.8
  • 13
    • 0035821594 scopus 로고    scopus 로고
    • Solid-phase synthesis of a nonpeptide RGD mimetic library: New selective αvβ3 integrin antagonists
    • Sulyok GAG, Gibson C, Goodman SL, Holzemann G, Wiesner M, Kessler H: Solid-phase synthesis of a nonpeptide RGD mimetic library: New selective αvβ3 integrin antagonists. J Med Chem (2001) 44:1938-1950.
    • (2001) J Med Chem , vol.44 , pp. 1938-1950
    • Sulyok, G.A.G.1    Gibson, C.2    Goodman, S.L.3    Holzemann, G.4    Wiesner, M.5    Kessler, H.6
  • 14
    • 0035825346 scopus 로고    scopus 로고
    • Inhibition of BCRP-mediated drug efflux by fumitremorgin-type indolyl diketopiperazines
    • Van Loevezijn A, Allen JD, Schinkel AH, Koomen G-J: Inhibition of BCRP-mediated drug efflux by fumitremorgin-type indolyl diketopiperazines. Bioorg Med Chem Lett (2001) 11:29-32.
    • (2001) Bioorg Med Chem Lett , vol.11 , pp. 29-32
    • Van Loevezijn, A.1    Allen, J.D.2    Schinkel, A.H.3    Koomen, G.-J.4
  • 15
    • 0034219844 scopus 로고    scopus 로고
    • Solid-phase synthesis of tetrasubstituted pyrazoles, novel ligands for the estrogen receptor
    • Stauffer SR, Katzenellenbogen JA: Solid-phase synthesis of tetrasubstituted pyrazoles, novel ligands for the estrogen receptor. J Combinatorial Chem (2000) 2:318-329. Results suggest that certain tetrasubstituted pyrazoles have high affinity and potency as agonists and antagonists for the estrogen α-subtype receptor.
    • (2000) J Combinatorial Chem , vol.2 , pp. 318-329
    • Stauffer, S.R.1    Katzenellenbogen, J.A.2
  • 18
    • 3543056384 scopus 로고    scopus 로고
    • Solid- and solution-phase synthesis of vancomycin and vancomycin analogues with activity against vancomycin-resistant bacteria
    • Nicolaou KC, Cho SY, Hughes R, Winssinger N, Smethurst C, Labischinski H, Endermann R: Solid- and solution-phase synthesis of vancomycin and vancomycin analogues with activity against vancomycin-resistant bacteria. Chem Eur J (2001) 7:3798-3823. Results suggest that vancomycin derivatives, modified on one of the sugar residues, provide highly potent antibacterial agents effective against vancomycin-resistant bacteria.
    • (2001) Chem Eur J , vol.7 , pp. 3798-3823
    • Nicolaou, K.C.1    Cho, S.Y.2    Hughes, R.3    Winssinger, N.4    Smethurst, C.5    Labischinski, H.6    Endermann, R.7
  • 19
    • 0035900319 scopus 로고    scopus 로고
    • The development and application of a novel safety-catch linker for BOC-based assembly of libraries of cyclic peptides
    • Boume GT, Golding SW, McGeary RP, Meutermans WDF, Jones A, Marshall GR, Alewood PF, Smythe ML: The development and application of a novel safety-catch linker for BOC-based assembly of libraries of cyclic peptides. J Org Chem (2001) 66:7706-7713. Results indicate that through development of novel solid-phase strategies, large arrays of cyclic peptides can now be accessed.
    • (2001) J Org Chem , vol.66 , pp. 7706-7713
    • Boume, G.T.1    Golding, S.W.2    McGeary, R.P.3    Meutermans, W.D.F.4    Jones, A.5    Marshall, G.R.6    Alewood, P.F.7    Smythe, M.L.8
  • 20
    • 0035909633 scopus 로고    scopus 로고
    • Traceless solid-phase synthesis of 1,2,4-triazoles using a novel amine resin
    • Larsen SD, DiPaolo BA: Traceless solid-phase synthesis of 1,2,4-triazoles using a novel amine resin. Org Lett (2001) 3:3341-3344. Results indicate that the development of a novel solid-phase linker allows access to medicinally relevant 1,2,4-triazoles where two points of diversity have been introduced.
    • (2001) Org Lett , vol.3 , pp. 3341-3344
    • Larsen, S.D.1    DiPaolo, B.A.2
  • 21
    • 0035907472 scopus 로고    scopus 로고
    • Regio-reactive resin: A platform for orthogonal loading using the polymer backbone and cross-linker
    • Dickerson TJ, Reed NN, Janda KD: Regio-reactive resin: A platform for orthogonal loading using the polymer backbone and cross-linker. Bioorg Med Chem Lett (2001) 11:1507-1509.
    • (2001) Bioorg Med Chem Lett , vol.11 , pp. 1507-1509
    • Dickerson, T.J.1    Reed, N.N.2    Janda, K.D.3


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.