Studies on Antitumor-active 2, 3-Dioxopiperazine Derivatives. I. Degradation Products of 1-(2-Chloroethyl)-3-(4-substituted-2, 3-dioxo-1-piperazinyl)-alkyl-1-nitrosourea in Aqueous Solution

• Published in: Chemical & pharmaceutical bulletin Vol. 29; no. 2; pp. 386 - 389
• Main Authors: HORI, TAKAKO, YOSHIDA, CHOSAKU, MURAKAMI, SHOHACHI, KIBA, YASUO, TAKENO, RYUKO, NAKANO, JOJI, TSUDA, HISATSUGU, SAIKAWA, ISAMU
• Format: Journal Article
• Language: English
• Published: Japan The Pharmaceutical Society of Japan 1981; Japan Science and Technology Agency
• Subjects: Animals; Antineoplastic Agents - analysis; Antineoplastic Agents - therapeutic use; antitumor agent of new type; Carcinoma, Ehrlich Tumor - drug therapy; Drug Stability; Female; Mice; Nitrosourea Compounds - analysis; Nitrosourea Compounds - pharmacology; Piperazines - analysis; Piperazines - pharmacology; Solutions
• ISSN: 0009-2363; 1347-5223
• DOI: 10.1248/cpb.29.386

Degradation products of 1-(2-chloroethyl)-3-(4-substituted-2, 3-dioxo-1-piperazinyl)-alkyl-1-nitrosourea in aqueous solution were investigated. Among them, a symmetrical urea derivative, 1, 3-bis [4-(4-ethyl-2, 3-dioxo-1-piperazinyl) butyl] urea (3c), was found to have antitumor activity. A synthetic unsymmetrical urea derivative, 1-[2-(4-ethyl-2, 3-dioxo-1-piperazinyl) ethyl]-3-methylurea (4a), also showed antitumor activity against Ehrlich carcinoma (solid form).