[EN] SELECTIVELY DELIVERABLE ISATIN-BASED CYTOTOXIC AGENTS<br/>[FR] AGENTS CYTOTOXIQUES À BASE D'ISATINE POUVANT ÊTRE ADMINISTRÉS SÉLECTIVEMENT
申请人:UNIV WOLLONGONG
公开号:WO2008074078A1
公开(公告)日:2008-06-26
[EN] The invention relates to compounds comprising a cytotoxic isatin derivative conjugated to a cell targeting moiety via a spacer group. These conjugates allow the cytotoxic isatin derivaties to be targeted to particular cell and tissue types. The invention also relates to novel isatin derivatives, intermediates used in preparing the conjugates and method of using the conjugates. [FR] L'invention concerne des composés contenant un dérivé d'isatine cytotoxique conjugué à un groupe fonctionnel de ciblage cellulaire au moyen d'un groupe espaceur. Ces conjugués permettent de cibler les dérivés d'isatine cytotoxiques sur des types de cellules et de tissus particuliers. L'invention concerne également de nouveaux dérivés d'isatine, des intermédiaires employés dans la préparation des conjugués et un procédé d'utilisation des conjugués.
[EN] N-[(AMINOSULFONYL)PHENYL]-2-(1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDENE)-HYDRAZINECARBOTHIOAMIDE DERIVATIVES FOR TREATING CANCER AND IMMUNOLOGICAL DISORDERS<br/>[FR] DÉRIVÉS DE N-[(AMINOSULFONYL)PHÉNYL]-2-(1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDÈNE)-HYDRAZINECARBOTHIOAMIDE POUR LE TRAITEMENT DU CANCER ET DE TROUBLES IMMUNOLOGIQUES
申请人:ISTANBUL UNIV REKTORLUGU
公开号:WO2017099695A1
公开(公告)日:2017-06-15
N-[(aminosulfonyl)phenyl]-2-(1,2-dihydro-2-oxo-3H-indol-3-ylidene)-hydrazinecarbothioamide derivatives of the following formula (III) for treating cancer and immunological disorders. R5, R6 and R7 are each independently selected from hydrogen and a sulfonamide group, provided that at least one of R5, R6 or R7 is a sulfonamide group. The substituents R1 to R4 are each independently either hydrogen or one of the substituents defined in the claims.
An Investigation into the Cytotoxicity and Mode of Action of Some Novel <i>N</i>-Alkyl-Substituted Isatins
作者:Kara L. Vine、Julie M. Locke、Marie Ranson、Stephen G. Pyne、John B. Bremner
DOI:10.1021/jm0704189
日期:2007.10.1
studies indicated that the introduction of an aromatic ring with a one or three carbon atom linker at N1 enhanced the activity from that of the allyl, 2'-methoxyethyl, and 3'-methylbutyl N-substituted isatins. Furthermore, electron-withdrawing groups substituted at the meta or para position of the ring were favored over the orthoorientation. Of the 24 compounds screened, nine displayed sub-micromolar IC50