A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 38/07 (2006.01) A61K 31/4709 (2006.01) A61K 38/08 (2006.01) C07K 5/103 (2006.01) C07K 7/00 (2006.01) A61K 38/00 (2006.01)
Patent
CA 2430782
A process for the total synthesis of thiocoraline and BE-22179 establishes the relative and absolute stereochemistry of these compounds and enables the construction and characterization of a series of related analogues (see Figure 4). The mechanism for the bioactivity of thiocoraline, BE-22179 and their related analogues is charaterized. Thiocoraline, BE-22179, and their related analogues are disclosed to bind to DNA by high-affinity bisintercalation and are disclosed to exhibit exceptional cytotoxic activity.
La présente invention concerne un procédé permettant la synthèse totale de thiocoraline et de BE-22179 qui établit la stéréochimie relative et absolue de ces composés et permet la construction et la caractérisation d'une série d'analogues associés. L'invention permet de déterminer le mécanisme de la bioactivité de thiocoraline, de BE-22179 et de leurs analogues. L'invention concerne la thiocoraline, la BE-22179, et leurs analogues associés qui se lient à l'ADN par bisintercalation à haute affinité et présentant une activité cytotoxique exceptionnelle.
The Scripps Research Institute
Torys Llp
LandOfFree
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