Novel piperazinediones as antitumor agents.

Chemical modification of dipeptide mimetic azatyrosine led to a series of piperazinediones. Thirteen piperazinediones were synthesized and tested for their anticancer activity. This series of piperazinedione compounds exhibited potent anticancer activities against human disease-oriented cancer cell lines in NCI60 cancer screening (National Cancer Institute, USA).

Azatyrosinamides: novel RAS-related anticancer agents.

Background: We previously reported on the design and synthesis of novel azatyrosinamide derivatives selective for ras-transformed NIH3T3 cells and with improved toxicity over azatyrosine. This study was aimed at investigating the mechanism of action and the antitumour activity of these compounds in ras-transformed cells.

Materials And Methods: Nine azatyrosinamides were previously screened for anticancer activity in both wild-type and ras-transformed NIH3T3 cells; the most active compounds were further tested in vitro and in vivo.

The total synthesis of a ganglioside Hp-s1 analogue possessing neuritogenic activity by chemoselective activation glycosylation.

The total synthesis of ganglioside 2, an analogue of the ganglioside Hp-s1 (1) which displays neuritogenic activity toward the rat pheochromocytoma cell line PC-12 cell in the presence of nerve growth factor (NGF) with an effect (34.0%) greater than that of the mammalian ganglioside GM 1 (25.4%), was accomplished by applying a chemoselective-activation glycosylation strategy.