New fascaplysin-based CDK4-specific inhibitors: design, synthesis and biological activity.
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.
Aubry
Carine
C
Department of Chemistry, University of Leicester, Leicester LE1 7RH, UK. kin@le.ac.uk
Jenkins
Paul R
PR
Mahale
Sachin
S
Chaudhuri
Bhabatosh
B
Maréchal
Jean-Didier
JD
Sutcliffe
Michael J
MJ
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D051358:Cyclin-Dependent Kinase 4; D018844:Cyclin-Dependent Kinases / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D008958:Models, Molecular; D011518:Proto-Oncogene Proteins / Q000037:antagonists & inhibitors*; D014439:Tyramine / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000737:chemistry; D000644:Quaternary Ammonium Compounds; D002243:Carbolines; D007212:Indolizines
D000970:Antineoplastic Agents; D051358:Cyclin-Dependent Kinase 4; D018844:Cyclin-Dependent Kinases; D004791:Enzyme Inhibitors; D007211:Indoles; D011518:Proto-Oncogene Proteins; D014439:Tyramine; C069346:fascaplysine; D000644:Quaternary Ammonium Compounds; D002243:Carbolines; D007212:Indolizines