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pro vyhledávání: '"Laura Garuti"'
The diaryl urea is an important fragment/pharmacophore in constructing anticancer molecules due to its near-perfect binding with certain acceptors. The urea NH moiety is a favorable hydrogen bond donor, while the urea oxygen atom is regarded as an ex
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2668ab59839340d41d2b50826110f3b3
https://hdl.handle.net/11576/2688396
https://hdl.handle.net/11576/2688396
Publikováno v:
Current Medicinal Chemistry. 19:3937-3948
Polo-like kinases (PLKs) are a family of serine/threonine kinases that play crucial roles in multiple stages of mitosis. PLK1 is the most studied member of the family. It is overexpressed in a wide spectrum of cancer types and is a promising target i
Publikováno v:
Current Medicinal Chemistry. 17:2804-2821
Protein kinases represent an attractive target in oncology drug discovery. Most of kinase inhibitors are ATP-competitive and are called type I inhibitors. The ATP-binding pocket is highly conserved among members of the kinase family and it is difficu
Publikováno v:
Current medicinal chemistry. 22(6)
none 3 no The limitations of many mono-kinase inhibitors can be overcome by agents with multi-target action. An important advantage of targeting more than one kinase, is an increase in potency, due to the synergistic effect. Moreover, this approach c
Autor:
Laura Garuti, Giorgio Cantelli-Forti, Benedetta Brighenti, Francesca Maffei, Carmela Fimognari, Patrizia Hrelia, Silvia Burnelli
Publikováno v:
Mutation Research/Fundamental and Molecular Mechanisms of Mutagenesis. 397:293-301
A new series of 4-nitro-(imidazoles and pyrazoles) were synthesized as novel antimycotics and tested for their activation to mutagenic forms using Salmonella typhimurium TA98 and TA100, in the presence and in the absence of metabolic activation. TA10
Publikováno v:
European Journal of Medicinal Chemistry. 33:43-46
Some 3-substituted indole-triazin-4-ones were synthesized. Their antiproliferative activity against chronic myeloid leukaemia and non-Hodgkin lymphoma human cells was compared in vitro with that of daunorubicin. One compound appeared to be very effec
Publikováno v:
Current medicinal chemistry. 21(20)
Benzimidazole is a common kinase inhibitor scaffold and benzimidazole-based compounds interact with enzymes by multiple binding modes. In some cases, the benzimidazole acts as part of the hinge-binding motif, in others it has a scaffolding role witho
Publikováno v:
Synthesis. 1994:1437-1440
Targeting cancer with small molecule irreversible inhibitors of kinases represents an emerging challenge in drug discovery. Irreversible inhibitors bind to kinase active site in a covalent and irreversible form, most frequently by reacting with a nuc
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b1d67e23b5e5ddec19f0541ac27f65bc
https://hdl.handle.net/11576/2688468
https://hdl.handle.net/11576/2688468
Publikováno v:
ChemInform. 22