Water-soluble antitumor agents. I. Synthesis and biological activity of 6-S-aminoacyloxymethyl mercaptopurine derivatives
| Autor: | Mitsuya Hongu, Naoko Narasaki, Tatsuo Kashida, Kouji Oda, Naoyuki Harada, Takashi Tanaka, Motoaki Ohohashi, Kenji Tsujihara, T. Hashiyama |
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| Rok vydání: | 1995 |
| Předmět: |
Magnetic Resonance Spectroscopy
medicine.drug_class Fibrosarcoma Antineoplastic Agents Tumor immunity Immunostimulant Chemical synthesis Mice Drug Discovery medicine Animals Mice Inbred BALB C Antitumor immunity Chemistry Mercaptopurine Water Biological activity Sarcoma General Chemistry General Medicine Bioavailability Water soluble Biochemistry Solubility Colonic Neoplasms Neoplasm Transplantation medicine.drug |
| Zdroj: | Chemicalpharmaceutical bulletin. 43(10) |
| ISSN: | 0009-2363 |
| Popis: | 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 derivatives (7a, b and 9a, b), were synthesized. These compounds were evaluated for activity to augment antitumor immunity by using a double grafted 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. |
| Databáze: | OpenAIRE |
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