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CEP-18770: A novel, orally active proteasome inhibitor with a tumor-selective pharmacologic profile competitive with bortezomib.
TLDR
Evidence is provided for the utility of CEP-18770 as a novel orally active proteasomesome inhibitor with a favorable tumor selectivity profile for the treatment of MM and other malignancies responsive to proteasome inhibition.
Discovery of a potent, selective, and orally active proteasome inhibitor for the treatment of cancer.
TLDR
The potent, selective, and orally bioavailable threonine-derived 20S human proteasome inhibitor that has been advanced to preclinical development, [(1R)-1-[[(2 S,3 R)-3-hydroxy-2]-1-oxobutyl]amino]-3-methylbutyl]boronic acid 20 (CEP-18770), is disclosed.
Reduced glutathione protects against cisplatin-induced neurotoxicity in rats.
TLDR
It is concluded that GSH prevents cisplatin-induced neuropathy and that it should be investigated further in the clinic.
Bbr 2778, an Aza-anthracenedione Endowed with Preclinical Anticancer Activity and Lack of Delayed Cardiotoxicity
TLDR
Although against in vivo models BBR 2778 was less potent than mitoxantrone and doxorubicin, its antitumor activity was equal or superior (in certain tumor models) to that of the above standard compounds.
A novel 7-modified camptothecin analog overcomes breast cancer resistance protein-associated resistance in a mitoxantrone-selected colon carcinoma cell line.
TLDR
A lipophilic 7-modified camptothecin analogue (ST1481) displayed a complete lack of cross-resistance in HT29/MIT cells, suggesting that the drug was not a substrate for BCRP because no defects in intracellular accumulation were found.
A novel trinuclear platinum complex overcomes cisplatin resistance in an osteosarcoma cell system.
TLDR
The ability of the triplatinum complex to overcome cisplatin resistance appears to be related to a different mechanism of DNA interaction (formation of different types of drug-induced DNA lesions) as compared with conventional mononuclear complexes rather than the ability to overcome specific cellular alterations.
BBR 3464: a novel triplatinum complex, exhibiting a preclinical profile of antitumor efficacy different from cisplatin.
TLDR
The profile of sensitivity to BBR 3464 within the 60-cell-lines screening panel of the National Cancer Institute, NIH differed from those of established drugs, thus supporting the hypothesis of a distinct mechanism of cytotoxic activity of B BR 3464.
Biological profile of FCE 24517, a novel benzoyl mustard analogue of distamycin A.
TLDR
In vivo and in vitro, FCE 24517 was found to possess evident antineoplastic activity on a series of murine transplanted solid tumours and human tumour xenografts and the following neoplasms were in fact found to be sensitive to FCE24517 treatment.
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