Nitrile-based peptoids as cysteine protease inhibitors.

Peptidomimetics of the class of dipeptidyl nitrile analog peptoids were synthesized as inhibitors of mammalian cysteine proteases of the papain superfamily. The dipeptidyl nitrile side chains were attached to the peptide backbone's nitrogen atom, not to the α-carbons. Synthesized nitrile-based peptoid analogs that lack the hydrogen amide at P2-P3 are responsible for many of the secondary structure elements in peptides and proteins, making them resistant to proteolysis.

A phase II study of mitoxantrone.

Thirty pretreated patients with progressive and measurable solid tumors (24/30 patients) or myeloproliferative diseases (6/30 patients) were given mitoxantrone at the dose of 5 mg/m2/day in 250 ml normal saline over 30 minutes infusion for 3 consecutive days every 3 weeks. A total of 104 cycles were administered, median 3 for each patient. 39/104 cycles were delayed for a median of 9 days (from 2 to 59 days) because of myelodepression grade I to III (median I); no infection or bleeding was observed.

[Cyclophosphamide, adriamycin and platinum (CAP) in the preoperative neoadjuvant phase and the therapy phase].

Forty-two patients with metastasized, and 7 patients with locally advanced forms of carcinoma of the breast were treated with a combination of three drugs: CTX 200-400 mg/sq.m. on days 1, 3 and 5, ADM 40 mg/sq.