58324-17-7Relevant academic research and scientific papers
Structure-activity relationships in the acronycine and benzo[b]acronycine series: Role of the pyran ring
Do, Quyen,Thi Mai, Huong Doan,Gaslonde, Thomas,Pfeiffer, Bruno,Leonce, Stephane,Pierre, Alain,Michel, Sylvie,Tillequin, Francois,Dufat, Hanh
experimental part, p. 2677 - 2687 (2009/04/11)
In order to explore the structure-activity relationships in the acronycine series, simplified analogues of cis-1,2-diacetoxy-1,2-dihydroacronycine and cis-1,2-diacetoxy-1,2-dihydrobenzo[b]acronycine (S23906-1, under clinical trials) lacking the fused pyran ring, but possessing an acetoxymethyl leaving group at position 4 were prepared. These new analogues only displayed marginal antiproliferative activity compared to the parent compounds. The presence of the angularly fused dimethylpyran ring appears as an indispensable structural requirement to observe significant cytotoxic activity in this series.
Structure-activity relationships in a series of anti-inflammatory N-arylanthranilic acids
Kaltenbronn,Scherrer,Short,Jones,Beatty,Saka,Winder,Wax,Williamson
, p. 621 - 627 (2007/10/02)
A large series of N-arylanthranilic acids has been prepared. Many of these compounds show high anti-inflammatory activity as measured by the anti-UV-erythema test. From this series have come the clinically useful nonsteroidal anti-inflammatory agents, flufenamic acid (Arlef), mefenamic acid (Ponstel), and the latest and most potent agent, N-(2,6-dichloro-m-tolyl)anthranilic acid (meclofenamic acid, Meclomen = the sodium salt). The structure-activity relationships of this series is discussed and a graphical representation is presented which allows the prediction of activity of new agents.
Structure activity relationships in centrally stimulating xanthone derivatives. Introduction to Parts X-XII, and Part X. Acridone derivatives
Valenti,Borraccini,Da Re,Cima
, p. 387 - 389 (2007/10/08)
Aspects of the structure activity relationships amongst the CNS stimulating xanthone derivatives 1 a to e were examined. These were: the bioisosteric replacement of the heterocyclic ring oxygen by an NH group (acridone derivatives, Part X); the lengthening of the amino methyl chain by one and 2 methylene groups as well as the locking of the basic chain and the methoxy group of 1 in a rigid structure (Part XI) and the preparation of some open models related to the first part (Part XII). All these modifications cause a lowering of the CNS stimulating activity as well as a change of the stimulating pattern from type 1 to type 2. Some conclusive remarks are presented and the critical sizes of a possible receptor site involved in the CNS stimulating activity of these types of compounds are tentatively suggested.
