[Conjugates of 2',3'-didehydro-3'-deoxythymidine with thymogen. Synthesis and anti-HIV activity].
An effective synthesis of thymogen was developed. Conjugates of 2',3'-didehydro-3'-deoxythymidine (nucleoside d4T) with thymogen were prepared in which the nucleoside hydroxyl group was linked to the thymogen carboxyl group of either tryprophan or glutamic acid residues. It was shown that the anti-HIV activity of the d4T-thymogene conjugate with the tryptophan linkage was comparable to that of d4T, whereas its cytotoxicity was nil. The d4T-tryptophan conjugate also displayed high anti-HIV activity.
Riakhovskiĭ
V V
VV
State Research Institute of Organic Chemistry and Technology, Moscow, Russia.
Malekin
S I
SI
Nosova
V M
VM
Kisin
A V
AV
Krugliak
Iu L
IuL
Kurochkin
V K
VK
D000163:Acquired Immunodeficiency Syndrome / Q000188:drug therapy*; D019380:Anti-HIV Agents / Q000737:chemistry* / Q000494:pharmacology*; D004151:Dipeptides; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D010455:Peptides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D018119:Stavudine / Q000737:chemistry* / Q000494:pharmacology*
D019380:Anti-HIV Agents; D004151:Dipeptides; D010455:Peptides; C060736:thymogen; D018119:Stavudine