Potential antitumor agents. 53. Synthesis, DNA binding properties, and biological activity of perimidines designed as minimal DNA-intercalating agents
摘要:
A series of compounds based on perimidine have been synthesized and evaluated for their DNA-binding properties and antitumor activity. The fused tricyclic permidine chromophore appears to be the minimal structural requirement for intercalative binding to DNA since the mode of binding could be dictated by the position of attachment of the side chain. The intercalating compounds have DNA association constants (log K = 5.8-6.5) and cytotoxic potencies (IC50 = 500-1500 nM) comparable to those shown by other classes of linear, tricyclic DNA-intercalating antitumor agents (acridinecarboxamides, phenazinecarboxamides), but none of the compounds showed in vivo activity.
POZHARSKIJ A. F.; KOMISSAROV I. V.; FILIPPOV I. T.; KONSTANTINCHENKO A. A+, XIM.-FARMATSEVT. ZH., 1977, 11, HO 5, 87-93
作者:POZHARSKIJ A. F.、 KOMISSAROV I. V.、 FILIPPOV I. T.、 KONSTANTINCHENKO A. A+
DOI:——
日期:——
KOMISSAROV I. V.; KONSTANTINCHENKO A. A.; POZHARSKIJ A. F.; FILIPPOV I. T+, XIM.-FARMATSEVT. ZH. <KNFZ-AN>, 1976, 10, HO 7, 28-33
作者:KOMISSAROV I. V.、 KONSTANTINCHENKO A. A.、 POZHARSKIJ A. F.、 FILIPPOV I. T+
DOI:——
日期:——
[EN] OXIDATIVE DYEING COMPOSITION COMPRISING A SPECIFIC PERIMIDINE COUPLER IN A MEDIUM WITH HIGH FATTY SUBSTANCE CONTENT, METHODS AND SUITABLE DEVICE<br/>[FR] COMPOSITION DE COLORATION D'OXYDATION COMPRENANT UN COUPLEUR PERIMIDINE SPÉCIFIQUE DANS UN MILIEU À TENEUR ÉLEVÉE EN CORPS GRAS, PROCÉDÉS ET DISPOSITIF ADAPTÉ
申请人:OREAL
公开号:WO2013087634A2
公开(公告)日:2013-06-20
Oxidative dyeing composition comprising a specific perimidine coupler in a medium with high fatty substance content, methods and suitable device The present invention relates to an oxidative dyeing composition for keratin fibres, in particular human keratin fibres such as the hair, comprising: - at least 25% by weight, relative to the total weight of the composition, of one or more fatty substances, - one or more surfactants, - one or more alkaline agents, - one or more oxidation bases, and - one or more perimidine couplers chosen from compounds having the following formula (I), their addition salts, their isomers, their tautomers, their solvates and their dimers: The invention also relates to methods using the composition according to the invention and to a multi-compartment device.
Potential antitumor agents. 53. Synthesis, DNA binding properties, and biological activity of perimidines designed as minimal DNA-intercalating agents
作者:John M. Herbert、Paul D. Woodgate、William A. Denny
DOI:10.1021/jm00394a025
日期:1987.11
A series of compounds based on perimidine have been synthesized and evaluated for their DNA-binding properties and antitumor activity. The fused tricyclic permidine chromophore appears to be the minimal structural requirement for intercalative binding to DNA since the mode of binding could be dictated by the position of attachment of the side chain. The intercalating compounds have DNA association constants (log K = 5.8-6.5) and cytotoxic potencies (IC50 = 500-1500 nM) comparable to those shown by other classes of linear, tricyclic DNA-intercalating antitumor agents (acridinecarboxamides, phenazinecarboxamides), but none of the compounds showed in vivo activity.
SHEJNKMAN A. K.; POZHARSKIJ A. F.; SOKOLOV V. I.; STUPNIKOVA T. V., DOKL. AN CCCP <DANK-AS>, 1976, 226, HO 5, 1094-1096
作者:SHEJNKMAN A. K.、 POZHARSKIJ A. F.、 SOKOLOV V. I.、 STUPNIKOVA T. V.