alpha-chymotrypsin has been researched along with 3--amino-2--3--dideoxycytidine* in 1 studies
1 other study(ies) available for alpha-chymotrypsin and 3--amino-2--3--dideoxycytidine
| Article | Year |
|---|---|
Synthesis and antileukemic activity of chymotrypsin-activated derivatives of 3'-amino-2',3'-dideoxycytidine. (Synthetic nucleosides and nucleotides. XXXIII.
3'-Amino-2',3'-dideoxycytidine (8) was directly synthesized from 2'-deoxycytidine. 2',3'-Dideoxy-3'-(N-acyl-L-phenylalanylamino)cytidines (acyl = butoxycarbonyl (9a), acetyl (9b), benzoyl (9c), and n-hexanoyl (9d)) were synthesized as chymotrypsin-activated prodrugs of 8. This N-protection was required for activation by chymotrypsin to 8. In vitro, compound 8 showed high cytotoxic activity against P388 cells, but the prodrugs 9a-d were ineffective. In vivo, however, these prodrugs showed much higher activity than 8 in mice bearing P388 cells. Topics: Animals; Antineoplastic Agents; Biotransformation; Chymotrypsin; Deoxycytosine Nucleotides; Leukemia P388; Mice; Zalcitabine | 1995 |