824409-50-9Relevant academic research and scientific papers
Design and synthesis of a focused library of novel aryl- and heteroaryl-ketopiperazides
Gerlach, Matthias,Claus, Eckhard,Baasner, Silke,Mueller, Gilbert,Polymeropoulos, Emmanuel,Schmidt, Peter,Guenther, Eckhard,Engel, Juergen
, p. 695 - 703 (2004)
1-Phenyl-4-piperazinyl-carbonyl-substituted nitrogen-containing heterocycles were discovered at Zentaris as a new class of potent, synthetic, small molecule tubulin inhibitors with strong antiproliferative activity. The lead structure of this class, D-24203, proved to be a potent inhibitor of in vivo tumor growth in different xenograft models including mammary and renal cancers. As part of our efforts in the lead optimization process to expand structural diversity as well as to optimize bioavailability parameters such as solubility and metabolic stability for these compounds, we produced and evaluated a focused library containing 320 compounds. Five new heterocyclic compound classes with comparable activity properties in the cytotoxicity and tubulin polymerization assay could be identified. In silico calculated bioavailability parameters for selected library members provides new compound classes with improved solubility properties. Library design, development of adequate solution phase methodology, and synthesis will be presented, as well as results of lead optimization.
Acridine derivatives and their use as medicaments
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Page/Page column 9, (2010/02/10)
The invention relates to novel acridine derivatives of the formula 1, to their preparation and to their use as medicaments, in particular for the treatment of tumors.
NOVEL ACRIDINE DERIVATIVES AND USE THEREOF AS MEDICAMENTS
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Page/Page column 22; 23, (2010/02/10)
The invention relates to novel acridine derivatives of general formula (I), the production and use thereof as medicaments, in particular, for the treatment of tumours.
