89180-99-4Relevant articles and documents
ALKYLBORONIC ACIDS AS ARGINASE INHIBITORS
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, (2020/08/22)
Provided are alkylboronic acids as arginase inhibitors represented by formula (I), or a pharmaceutically acceptable salt, stereoisomer, tautomer, or prodrug thereof and a pharmaceutical composition comprising said compounds.
Molecular modelling studies, synthesis and biological activity of a series of novel bisnaphthalimides and their development as new DNA topoisomerase II inhibitors
Filosa, Rosanna,Peduto, Antonella,Di Micco, Simone,Caprariis, Paolo de,Festa, Michela,Petrella, Antonello,Capranico, Giovanni,Bifulco, Giuseppe
scheme or table, p. 13 - 24 (2011/02/25)
A series of bisnaphthalimide derivatives were synthesized and evaluated for growth-inhibitory property against HT-29 human colon carcinoma. The N,N′-bis[2-(5-nitro-1,3-dioxo-2,3-dihydro-1H-benz[de]-isoquinolin- 2-yl)]propane-2-ethanediamine (9) and the N,N′-Bis[2-(5-nitro-1,3-dioxo-2,3-dihydro-1H-benz[de]-isoquinolin- 2-yl)]butylaminoethyl]-2-propanediamine (12) derivatives emerged as the most potent compounds of this series. Molecular modelling studies indicated that the high potency of 12, the most cytotoxic compound of the whole series, could be due to larger number of intermolecular interactions and to the best position of the naphthalimido rings, which favours π-π stacking interactions with purine and pyrimidine bases in the DNA active site. Moreover, 12 was designed as a DNA topoisomerase II poison and biochemical studies showed its effect on human DNA topoisomerase II. We then selected the compounds with a significant cytotoxicity for apoptosis assay. Derivative 9 was able to induce significantly apoptosis (40%) at 0.1 μM concentration, and we demonstrated that the effect on apoptosis in HT-29 cells is mediated by caspases activation.
Novel bisbenzamidines as potential drug candidates for the treatment of Pneumocystis carinii pneumonia
Vanden Eynde, Jean Jacques,Mayence, Annie,Huang, Tien L.,Collins, Margaret S.,Rebholz, Sandra,Walzer, Peter D.,Cushion, Melanie T.
, p. 4545 - 4548 (2007/10/03)
A series of pentamidine congeners has been synthesized and screened for their in vitro activity against Pneumocystis carinii. Among the tested compounds, bisbenzamidines linked by a flexible pentanediamide or hexanediamide chain (7 and 9) emerged as excep