Abstract:
:A series of carbamides derived from 1,2:5,6-di-O-isopropylidene-D-gluco- and D-allofuranose as well as their 5,6-O-deprotected analogues (2 and 4) and methyl 3,4-O-isopropylidene-alpha- and beta-D-galactopyranosides (5 and 6) have been prepared in order to evaluate their ability to induce erythroid differentiation of human erythroleukemic K562 cells. Twenty out of 51 carbamides tested exhibit an appreciable activity as inducers of erythroid differentiation and have been fully characterized and described.
journal_name
Eur J Med Chemjournal_title
European journal of medicinal chemistryauthors
Landi M,Catelani G,D'Andrea F,Ghidini E,Amari G,Paola P,Bianchi N,Gambari Rdoi
10.1016/j.ejmech.2008.05.001subject
Has Abstractpub_date
2009-02-01 00:00:00pages
745-54issue
2eissn
0223-5234issn
1768-3254pii
S0223-5234(08)00264-Xjournal_volume
44pub_type
杂志文章abstract::A series of newly asymmetric dimeric β-carbolines with a spacer of 4-6 methylene units between the indole nitrogen and the harmine oxygen were synthesized. Structures of all the novel synthesized compounds were confirmed by their spectral and analytical studies. All of the synthesized compounds were screened for their...
journal_title:European journal of medicinal chemistry
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journal_title:European journal of medicinal chemistry
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journal_title:European journal of medicinal chemistry
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abstract::Selective kinase inhibitors development is a cumbersome task because of ATP binding sites similarities across kinases. On contrast, irreversible allosteric covalent inhibition offers opportunity to develop novel selective kinase inhibitors. Previously, we reported thiazolidine-2,4-dione lead compounds eliciting in vit...
journal_title:European journal of medicinal chemistry
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abstract::Axl is a new promising molecular target for antineoplastic therapies. A series of quinolone antibiotic derivatives were designed and synthesized as new selective Axl inhibitors. One of the most promising compound 8i bound tightly to Axl with a Kd value of 1.1 nM, and inhibited its kinase activity with an IC50 value of...
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abstract::Twelve novel substituted isatin-propylene-1H-1,2,3-triazole-4-methylene-moxifloxacin hybrids 5a-l were designed, synthesized and screened for their in vitro anti-mycobacterial activities against drug-sensitive and multidrug-resistant Mycobacterium tuberculosis as well as cytotoxicity in VERO cell line. All hybrids exh...
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abstract::The coagulation factor Xa (FXa) plays a central role in the blood coagulation cascade. Recent studies have shown that FXa is a particularly attractive target for the development of oral antithrombotic agents. In view of the excellent pharmaceutical properties of 1,2-phenylenediamine-based FXa inhibitors and the report...
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abstract::Spiro derivatives of oxindole and isoxazole-5-one were synthesized by using Michael addition reaction, highlighting the regioselective approach towards the synthesis of Michael diadduct followed by condensation of Michael diadduct. The spiro compound 4 showed antitubercular activity against Mycobacterium tuberculosis ...
journal_title:European journal of medicinal chemistry
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journal_title:European journal of medicinal chemistry
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journal_title:European journal of medicinal chemistry
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journal_title:European journal of medicinal chemistry
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更新日期:2018-02-10 00:00:00