176-33-0Relevant articles and documents
HETEROCYCLIC COMPOUND
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Page/Page column 62, (2013/02/28)
Provided is a compound useful for the prophylaxis or treatment of cancer. The present invention relates to a compound represented by formula (I): wherein each symbol in the formula is as defined in the specification, or a salt thereof or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer.
Design, synthesis, and biological evaluation of 14-substituted aromathecins as topoisomerase I inhibitors
Cinelli, Maris A.,Morrell, Andrew,Dexheimer, Thomas S.,Scher, Evan S.,Pommier, Yves,Cushman, Mark
experimental part, p. 4609 - 4619 (2009/07/04)
The aromathecin or "rosettacin" class of topoisomerase I (top1) inhibitors is effectively a "composite" of the natural products camptothecin and luotonin A and the synthetic indenoisoquinolines. The aromathecins have aroused considerable interest following the isolation and total synthesis of 22-hydroxyacuminatine, a rare cytotoxic natural product containing the 12H-5,11a-diazadibenzo[b,h]fluoren-11-one system. We have developed two novel syntheses of this system and prepared a series of 14-substituted aromathecins as novel antiproliferative topoisomerase I poisons. These inhibitors are proposed to act via an intercalation and "poisoning" mechanism identical to camptothecin and the indenoisoquinolines. Many of these compounds possess greater antiproliferative activity and anti-top 1 activity than the parent unsubstituted compound (rosettacin) and previously synthesized aromathecins, as well as greater top1 inhibitory activity than 22-hydroxyacuminatine. In addition to potentially aiding solubility and localization to the DNA-enzyme complex, nitrogenous substituents located at the 14-position of the aromathecin system have been proposed to project into the major groove of the top1-DNA complex and hydrogen-bond to major-groove amino acids, thereby stabilizing the ternary complex.
AMINOCYCLOHEXYL ETHER COMPOUNDS AND USES THEREOF
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Page 26, (2008/06/13)
Aminocyclohexyl ether compounds of formula (I), or a solvate or pharmaceutically acceptable salt thereof: are disclosed. In said formula, A, X and R, -R5 have the meanings given in the description. The compounds of the present invention may be inco