Synthesis of imidazo[2,1-a]phthalazines, potential inhibitors of p38 MAP kinase.: Prediction of binding affinities of protein Ligands

被引:0
|
作者
Mavel, S [1 ]
Thery, I [1 ]
Gueiffier, A [1 ]
机构
[1] Fac Pharm, Chim Therapeut Lab, F-37200 Tours, France
关键词
imidazophthalazine; Suzuki coupling; molecular modeling; p38; MAPK;
D O I
10.1002/1521-4184(200201)335:1<7::AID-ARDP7>3.0.CO;2-L
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Based upon molecular modeling, the pharmacophore of potential inhibitors of p38 MAPK (mitogen-activated protein kinases) is discussed and the predictive binding affinities are calculated. Syntheses of original diarylimidazo[2,1-a]phthalazines obtained by Suzuki coupling are described.
引用
收藏
页码:7 / 14
页数:8
相关论文
共 50 条
  • [1] Allosteric and slow binding inhibitors of p38 MAP kinase.
    Regan, J
    Breitfelder, S
    Cirillo, P
    Gilmore, T
    Graham, A
    Hickey, E
    Madwed, J
    Moriak, M
    Moss, N
    Pargellis, C
    Proto, A
    Tong, L
    Torcellini, C
    [J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2001, 222 : U683 - U683
  • [2] Novel inhibitors of p38 MAP kinase.
    Shetty, R
    Moffett, KK
    Nguyen, D
    Kelly, MJ
    Michelotti, EL
    Dorsey, BD
    Springman, E
    Bukhtiyarova, M
    Northrop, K
    Chai, XM
    Saporito, MS
    Ochman, AR
    Karpusas, M
    [J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2004, 228 : U947 - U947
  • [3] PRK, a novel protein kinase regulated by the p38 MAP kinase.
    New, T
    Jiang, Y
    Zhao, M
    Liu, K
    Flood, L
    Kato, Y
    Parry, G
    Han, J
    [J]. FASEB JOURNAL, 1998, 12 (04): : A448 - A448
  • [4] Effects of Water Placement on Predictions of Binding Affinities for p38α MAP Kinase Inhibitors
    Luccarelli, James
    Michel, Julien
    Tirado-Rives, Julian
    Jorgensen, William L.
    [J]. JOURNAL OF CHEMICAL THEORY AND COMPUTATION, 2010, 6 (12) : 3850 - 3856
  • [5] Discovery and design of novel benzimidazolone as inhibitors of p38 MAP kinase.
    Hammach, A
    Ralph, M
    Corbo, F
    Barbosa, A
    Liu, PR
    Soleymanzadeh, F
    Goldberg, D
    Sarko, C
    Mckibben, B
    Moss, N
    Hao, MH
    White, A
    Qian, K
    Pargellis, C
    Kroe, R
    Wildeson, J
    Nelson, R
    Fadra, T
    Capolino, A
    Kashem, M
    Patnaude, L
    Madwed, J
    Torcellini, C
    Kaplita, P
    Farrel, T
    Hu, HB
    Yazdania, M
    Kavanaugh, K
    [J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2004, 228 : U947 - U947
  • [6] 4-azaindoles: Novel inhibitors of p38 MAP kinase.
    Trejo, A
    Arzeno, H
    Browner, M
    Cheng, SA
    Corner, DD
    Dalrymple, S
    Freire-Moar, J
    Lim, J
    Mcintosh, J
    Miller, J
    Myers, PL
    Saunders, J
    Sjogren, EB
    Spellmyer, D
    Warren, SD
    Whiteley, PE
    Zeng, L
    Goldstein, DM
    [J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2002, 224 : U59 - U59
  • [7] Synthesis and biological evaluation of BIRB 796 analogs as potent inhibitors of p38 MAP kinase.
    Swinamer, AD
    Capolino, A
    Cirillo, PF
    Gilmore, T
    Graham, A
    Hickey, E
    Moriak, M
    Madwed, J
    Moss, N
    Nelson, R
    Pargellis, C
    Regan, J
    Torcellini, C
    Tsang, M
    [J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2002, 224 : U59 - U60
  • [8] Structure active relationship of substituted imidazo(2,1-b)thiazoles:: Novel, selective p38 MAP kinase inhibitors
    Vensel, D
    Ashwell, MA
    Ali, SM
    Antonenko, V
    Graceffa, R
    Harris, M
    Kaselj, M
    Kelleher, E
    Liu, J
    Lapierre, JM
    Liu, Y
    O'Donnell, M
    Selliah, R
    Tandon, M
    Wrona, W
    Bresciano, K
    Caserta, K
    Chan, H
    Gannett, T
    Jones, S
    Leydon, P
    Mcdonald, S
    Naper, A
    Saraswat, L
    Tyler, A
    Warren, M
    Zhu, S
    [J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2005, 230 : U2723 - U2723
  • [9] C7-substituted quinazolinone and dihydroquinazolinone inhibitors of p38 map kinase.
    Bao, JM
    Miao, SW
    Rupprech, KM
    Pivnichny, JV
    Zaller, DM
    Shoop, WL
    O'Neill, EA
    O'Keefe, SJ
    Thompson, CM
    Cubbon, RM
    Wang, RX
    Zhang, WX
    Thompson, JE
    Doherty, JB
    [J]. ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2005, 229 : U130 - U130
  • [10] Synthesis and Evaluation of Pyridinyltriazoles as Inhibitors of p38 MAP Kinase
    Moallem, Seyed Adel
    Hadizadeh, Farzin
    Abadi, Fatemeh Abdol
    Shahraki, Mahmoud
    Shamsara, Jamal
    [J]. IRANIAN JOURNAL OF BASIC MEDICAL SCIENCES, 2012, 15 (04) : 945 - 950