New fascaplysin-based CDK4-specific inhibitors:: design, synthesis and biological activity

被引:32
作者
Aubry, C
Jenkins, PR [1 ]
Mahale, S
Chaudhuri, B
Maréchal, JD
Sutcliffe, MJ
机构
[1] Univ Leicester, Dept Chem, Leicester LE1 7RH, Leics, England
[2] De Montfort Univ, Sch Pharm, Leicester LE1 9BH, Leics, England
[3] Univ Leicester, Dept Biochem & Chem, Leicester LE1 7RH, Leics, England
关键词
D O I
10.1039/b406076h
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
The first biologically active non-planar analogues of the toxic anti-cancer agent, fascaplysin, have been produced; we present the design, synthesis and biological activity of three tryptamine derivatives.
引用
收藏
页码:1696 / 1697
页数:2
相关论文
共 21 条
[1]  
Alberts B, 2002, MOL CELL BIOL
[2]   Intramolecular inverse electron demand Diels-Alder reactions of tryptamine with tethered heteroaromatic azadienes [J].
Benson, SC ;
Lee, L ;
Yang, L ;
Snyder, JK .
TETRAHEDRON, 2000, 56 (09) :1165-1180
[3]   The Protein Data Bank [J].
Berman, HM ;
Westbrook, J ;
Feng, Z ;
Gilliland, G ;
Bhat, TN ;
Weissig, H ;
Shindyalov, IN ;
Bourne, PE .
NUCLEIC ACIDS RESEARCH, 2000, 28 (01) :235-242
[4]   Crystal structure of the complex of the cyclin D dependent kinase Cdk6 bound to the cell-cycle inhibitor p19INK4d [J].
Brotherton, DH ;
Dhanaraj, V ;
Wick, S ;
Brizuela, L ;
Domaille, PJ ;
Volyanik, E ;
Xu, X ;
Parisini, E ;
Smith, BO ;
Archer, SJ ;
Serrano, M ;
Brenner, SL ;
Blundell, TL ;
Laue, ED .
NATURE, 1998, 395 (6699) :244-250
[5]  
Clews J., 2000, J CHEM SOC P1, V24, P4306
[6]   A CARDIOSELECTIVE, HYDROPHILIC N,N,N-TRIMETHYLETHANAMINIUM ALPHA-TOCOPHEROL ANALOG THAT REDUCES MYOCARDIAL INFARCT SIZE [J].
GRISAR, JM ;
PETTY, MA ;
BOLKENIUS, FN ;
DOW, J ;
WAGNER, J ;
WAGNER, ER ;
HAEGELE, KD ;
DEJONG, W .
JOURNAL OF MEDICINAL CHEMISTRY, 1991, 34 (01) :257-260
[7]   DNA binding properties of the marine sponge pigment fascaplysin [J].
Hörmann, A ;
Chaudhuri, B ;
Fretz, H .
BIOORGANIC & MEDICINAL CHEMISTRY, 2001, 9 (04) :917-921
[8]   Small molecules as inhibitors of cyclin-dependent kinases [J].
Huwe, A ;
Mazitschek, R ;
Giannis, A .
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 2003, 42 (19) :2122-2138
[9]   Development and validation of a genetic algorithm for flexible docking [J].
Jones, G ;
Willett, P ;
Glen, RC ;
Leach, AR ;
Taylor, R .
JOURNAL OF MOLECULAR BIOLOGY, 1997, 267 (03) :727-748
[10]  
Kaelin WG, 1999, BIOESSAYS, V21, P950, DOI 10.1002/(SICI)1521-1878(199911)21:11<950::AID-BIES7>3.3.CO