Nitrosourea antitumor agents--correlation between antitumor action and some biochemical properties of newly synthesized derivatives (Meeting abstract).

Important note: Information in this article was accurate in 1993. The state of the art may have changed since the publication date.

Nitrosourea antitumor agents--correlation between antitumor action and some biochemical properties of newly synthesized derivatives (Meeting abstract).

Eighth Mediterranean Congress of Chemotherapy. May 24-9, 1992, Athens, Greece, p. 742-3, 1992. Unique Identifier : AIDSLINE ICDB/93688851
Illarionova M; Zheleva A; Raikov Z; Todorov D; Dudov; Natl. Oncological Center, Sofia, Bulgaria

Abstract: The nitrosourea derivatives from several groups (spin-labeled and nonspin-labeled 2-chloroethyl-nitrosourea derivatives of some amino acids as alanine, glycine, methionine, leucine and others) on the rational basis were synthesized. The antitumor activity and some related to that activity, and biochemical properties (alkylating and carbamoylating activity and half-life time) of newly synthesized nitrosoureas were studied. A strong relationship between antitumor activity and studied biochemical properties was found. The alanine-containing nitrosourea possessed an alkylating activity of 0.620, carbamoylating activity of 34.47% and T1/2 = 28 min, and an antitumor activity of T/C = 714.3%; the methionine-containing nitrosourea 0.850 for alkylating activity, 32.44% for carbamoylating activity, T1/2 = 25 min and T/C = 571.7% on BDF1-hybrid mice bearing L1210 lymphoid leukemia. The described experimental data showed that the approach of using some amino acids as carriers of nitrosourea groups was prospective for design of new generation nitrosourea agents.

Keywords: Antigens, CD/ANALYSIS Antigens, CD3/ANALYSIS Antigens, CD4/ANALYSIS Antigens, CD8/ANALYSIS Antigens, Differentiation, B-Lymphocyte/ANALYSIS Central Nervous System Neoplasms/IMMUNOLOGY/PATHOLOGY CD4-CD8 Ratio Human *Leukocyte Count Lung Neoplasms/IMMUNOLOGY/*PATHOLOGY Lymphocytes/*PATHOLOGY Mesothelioma/IMMUNOLOGY/PATHOLOGY Uterine Neoplasms/IMMUNOLOGY/PATHOLOGY MONOGRAPH
930430
M9340820

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