Universitá Degli Studi Di Padova

Hoffmann-la Roche Inc.

Giuseppe Zagotto

Siro Serafini

Modesto Carli

Teresa Pecere

Giovanni Ribaudo

Anna Maria Brunati

Mario Angelo Primo Pagano

Elena Tibaldi

Livio Trentin

Giorgio Palu

Giorgio Palu'

The present invention relates to a 1-phenylpropanone compound of formula (I), wherein X is CHor an atom selected from the group consisting of O, S and Se, n is an integer from 4 to 6, A is a substituent selected from the group consisting of 4-morpholyl, 1-piperidinyl, 4-methyl-1-piperazinyl, A being optionally substituted with a (C-C)alkyl or (C-C)acyl substituent, with the proviso that when X is CH, n is equal to 5, for use as an antitumoral agent in the treatment of breast cancer, chronic lymphatic leukemia or neuroblastoma. The invention also concerns new 1-phenylpropanone compounds, and compounds as antitumoral agents. 

1-phenylpropanone compounds and use thereof

The invention relates to aloe-emodin (AE) derivatives and their use as anticancer drugs. Saids derivatives show a specific cytotoxicity to tumour cells, also of neuroectodermal origin, to which they may in particular act as aloe-emodin prodrugs. Said pharamcological profile makes them particularly suitable for use in the treatment of neoplasias. Thereofore, pharmaceutical compositions containing said compound may be usefully used in the treatment of neoplasias. It has surprisingly been found that aloe-emodin derivatives in position 3' (bearing either a positive or negaive charge) exhibit improved sollubility properties and, at the same time, in vitro show cytotoxicity to tumour cells, also of neuroectodermal origin.

Aloe-emodin derivatives and their use in the treatment of neoplasias

4-Dimethylamino-3,5-dimethoxy-benzaldehyde, an intermediate for the preparation of the antibacterially active aditoprim (4-dimethylamino-3,5-dimethoxybenzoldehyde) a known antibacterially active compound, is obtained from 4-dimethylaminobenzonitrile by bromination or chlorination, replacement of the halogen by the methoxy group and reduction of the nitrile group.

Process for 4-dimethylamino-3,5-dimethoxybenzaldehyde

Growing community of inventors

Terrossa, Italy

Giuseppe Zagotto