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Water-soluble antitumor agents. I. Synthesis and biological activity of 6-S-aminoacyloxymethyl mercaptopurine derivatives.
- Source :
-
Chemical & pharmaceutical bulletin [Chem Pharm Bull (Tokyo)] 1995 Oct; Vol. 43 (10), pp. 1793-6. - Publication Year :
- 1995
-
Abstract
- In an attempt to improve the effectiveness and bioavailability of 6-mercaptopurine, various kinds of water-soluble analogues, such as 6-S-aminoacyloxymethyl mercaptopurine derivatives (3a--m) and 6-S,9-disubstituted derivates (7a,b and 9a,b), were synthesized. These compounds were evaluated for activity to augment antitumor immunity by using a double grated tumor system. Antitumor activities against solid tumors (sarcoma 180 and colon 26) were also evaluated. Many compounds exhibited potent activities in both test systems. In particular, the aminopropionate derivative (3a) and the L-glutamate derivative (3f) showed significant enhancement of antitumor immunity together with potent antitumor activities.
- Subjects :
- Animals
Antineoplastic Agents chemistry
Colonic Neoplasms pathology
Fibrosarcoma pathology
Magnetic Resonance Spectroscopy
Mercaptopurine analogs & derivatives
Mice
Mice, Inbred BALB C
Neoplasm Transplantation
Sarcoma pathology
Solubility
Water chemistry
Antineoplastic Agents chemical synthesis
Antineoplastic Agents pharmacology
Mercaptopurine chemical synthesis
Mercaptopurine pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 0009-2363
- Volume :
- 43
- Issue :
- 10
- Database :
- MEDLINE
- Journal :
- Chemical & pharmaceutical bulletin
- Publication Type :
- Academic Journal
- Accession number :
- 8536352
- Full Text :
- https://doi.org/10.1248/cpb.43.1793