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Due to their system of annulated 6-5-5-6-membered rings, indenoindoles have sparked great interest for the design of ATP-competitive inhibitors of human CK2. In the present study, we prepared twenty-one indeno[1,2-b]indole derivatives, all of which were tested in vitro on human CK2. The indenoindolones 5a and 5b inhibited human CK2 with an IC50 of 0.17 and… (More)
Ketonic indeno[1,2-b]indole-9,10-dione derivatives, initially designed as human casein kinase II (CK2) inhibitors, were recently shown to be converted into efficient inhibitors of drug efflux by the breast cancer resistance protein ABCG2 upon suited substitutions including a N (5)-phenethyl on C-ring and hydrophobic groups on D-ring. A series of ten… (More)
Artemether (AM) plus azithromycin (AZ) rectal co-formulations were studied to provide pre-referral treatment for children with severe febrile illnesses in malaria-endemic areas. The target profile required that such product should be cheap, easy to administer by non-medically qualified persons, rapidly effective against both malaria and bacterial… (More)
The GP2A European Conference is a two-day meeting focused on medicinal chemistry and the use of tools to explore all fields of drug discovery and drug design such as molecular modelling, bioorganic chemistry, MS studies, in vitro in vivo assays, and structure activity relationships. Abstracts of keynote lectures, plenary lectures, junior lectures, flash… (More)
In the crystal structure of the title compound, C16H24N4O4, mol-ecules are linked by N-H⋯O hydrogen bonds between the carbonyl groups of the carbamoyl and amido functional groups and the amino groups, and by N-H⋯N hydrogen bonds between the amino group and the pyridine ring, forming two-dimensional networks parallel to the ab plane.
Up to five different crystalline radical salts have been prepared with the organic donor BEDT-TTF and three different polynitrile anions. With the polynitrile dianion tcpd 2− (=C[C(CN) 2 ] 3 2−), two closely related radical salts: α'-(ET) 4 tcpd· THF (1) (THF = tetrahydrofurane) and α'-(ET) 4 tcpd· H 2 O (2) have been prepared, depending on the solvent used… (More)