Identification of inhibitors of DNA topoisomerase II from a synthetic library of glycoconjugates.
A library of 24 glycoconjugates related to glycosylated beta-amino acid derivative (I) was been prepared and screened against DNA topoisomerase-II of the filarial parasite S. cervi. Among these, compound 6 was found to be a potent inhibitor of DNA topoisomerase-II with 95% inhibition at 1.09 microM. Furthermore, compound 6 was at least three times more potent than the lead compound, glycosylated beta-amino acid derivative I.
Tripathi
R P
RP
Division of Medicinal Chemistry, Central Drug Research Institute, Lucknow, 226 001, India. Bijoy_Kundu@Yahoo.com
Rastogi
S K
SK
Kundu
B
B
Saxena
J K
JK
Reddy
V J
VJ
Srivastava
S
S
Chandra
S
S
Bhaduri
A P
AP
D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D015723:Gene Library; D006001:Glycoconjugates / Q000737:chemistry* / Q000494:pharmacology*; D059005:Topoisomerase II Inhibitors
D004791:Enzyme Inhibitors; D006001:Glycoconjugates; D059005:Topoisomerase II Inhibitors