Disease relevance of Dinaline

• The efficacy and toxicity of Acetyldinaline for remission-induction treatment of leukemia were evaluated and compared with those observed in previous studies of Dinaline in the Brown Norway acute myelocytic leukemia, as a preclinical model for human acute myelocytic leukemia [1].
• Dinaline: a new oral drug against leukemia? Preclinical studies in a relevant rat model for human acute myelocytic leukemia (BNML) [2].
• Dinaline [4-amino-N-(2'-aminophenyl)-benzamide, Din], p-N-methyldinaline (Me-Din) and p-N-acetyldinaline (Ac-Din) were evaluated for their antineoplastic efficacy in acetoxymethylmethylnitrosamine-induced colorectal carcinomas in Sprague-Dawley rats and in two human colon cancer cell lines [3].

High impact information on Dinaline

• OBJECTIVES: CI-994 (N-acetyl dinaline, PD 123654) is a novel oral agent active in a broad variety of murine and human tumor xenografts [4].
• The CI-994 AUC on D-1 and D-14 were 2879 and 2407 micrograms/ml x minutes, respectively; while the dinaline AUC on D-1 and D-14 were 87 and 92 micrograms/ml x minutes, respectively [5].
• The cytostatic and antiproliferative effect of dinaline, observed in cell growth curves, could be demonstrated by the impaired thymidine incorporation into DNA [6].
• METHODS: Bone marrow and spleen cells from untreated mice were continuously exposed in vitro to acetyldinaline or dinaline in clonal assays [7].
• The human colon carcinoma cell line SW 707 was exposed for up to 72 h to the new antineoplastic agent 4-amino-N-(2'-aminophenyl)benzamide (GOE 1734, dinaline) [8].

Biological context of Dinaline

• Combination treatment based on metabolic effects of dinaline [8].
• Since the cytostatic effect of dinaline could be enhanced by dGlc although incubation with dGlc alone caused no changes in cell number, the combined effect of both agents is synergistic [8].
• 24 h exposure to low concentrations of dinaline caused mild cell proliferation which turned into a cytostatic effect within a further 24 h without drug exposure [9].

Anatomical context of Dinaline

• The inhibition of the sodium-dependent uptake of AIB might indicate interaction of dinaline with cell membrane functions at low concentrations, the increase in methionine uptake points to enhanced protein synthesis following drug withdrawal and the impaired thymidine incorporation into DNA results from the cytostatic effect of dinaline [9].

Gene context of Dinaline

• For all periods of exposure a diminished S phase (3%-71% of control) was found initially after incubation, demonstrating the antiproliferative effect of dinaline, with total recovery after 1 day [8].

Analytical, diagnostic and therapeutic context of Dinaline

• It is the acetylated metabolite of dinaline, a compound previously identified as having cytotoxic and cytostatic activity against several murine and human xenograft tumor models [10].
• Up to 4 h after treatment of human SW 707 colon carcinoma cells with the antineoplastic drug 4-amino-N-(2'-aminophenyl)-benzamide (GOE 1734, dinaline), the effects of tumour cell metabolism and proliferation were examined in vitro [6].
• The long-term toxic risk of the cytostatic agent dinaline (4-amino-N-(2'-aminophenyl)-benzamide) was assessed in a rat bioassay [11].

References