Efficacy of dinaline and its methyl and acetyl derivatives against colorectal cancer in vivo and in vitro

European Journal of Cancer : Official Journal for European Organization for Research and Treatment of Cancer (EORTC) [and] European Association for Cancer Research (EACR)
M H Seelig, M R Berger

Abstract

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. Din was very effective at all dosages (10, 7.7 and 5.9 mg/kg) as indicated by the ratio of median tumour volume of treated and control groups (T/C%) values of 0.4, 16 and 10.6, respectively, but also caused a corresponding mortality of 87, 47 and 13%, respectively, as opposed to 15% in the control group. Me-Din also showed significant tumour growth inhibition at all dosages (13.8, 10.6, 8.2 and 6.2 mg/kg), as evidenced by T/C% values of 2, 5.7, 8.4 and 25, respectively. The corresponding mortality was 47, 20, 27 and 30%, respectively. Ac-Din showed the lowest mortality with 20, 13 and 20% at dosages of 9.1, 7.0 and 5.3 mg/kg, respectively, whereas application of 11.9 mg/kg resulted in 100% mortality. T/C values of 18.3, 11.1 and 21.6%, respectively, demonstrated again high anticancer efficacy. Compared to the combination therapy with 5-FU and leucovorin (25 mg/kg each), p-N-acetyldinaline (7.0 mg/kg) was 4-fold more effective as indicated by...Continue Reading

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Citations

Mar 12, 2004·Cancer Chemotherapy and Pharmacology·Donna A VolpeRalph E Parchment
Apr 1, 2004·Expert Opinion on Therapeutic Patents·Richard Warburg, Lauren Nguyen
Nov 3, 2004·Annals of Oncology : Official Journal of the European Society for Medical Oncology·S D UndeviaM J Ratain
Mar 14, 2007·Anti-cancer Drugs·Claude Monneret
Jul 2, 2019·Biomedit︠s︡inskai︠a︡ khimii︠a︡·K V ShevchenkoN F Myasoedov
Nov 14, 2003·Journal of Medicinal Chemistry·Thomas A MillerSandro Belvedere
Jan 12, 2005·European Journal of Medicinal Chemistry·Claude Monneret

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