摘要:
The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.
摘要:
One embodiment of the present invention is a method of treating a subject with a multi-drug resistant cancer. The method comprises administering to the subject an effective amount of a compound represented by Structural Formula (I): 1 Y is a covalent bond or a substituted or unsubstituted straight chained hydrocarbyl group, or, Y, taken together with both>CnullZ groups to which it is bonded, is a substituted or unsubstituted aromatic group. R1-R4 are independently nullH, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group, or R1 and R3 taken together with the carbon and nitrogen atoms to which they are bonded, and/or R2 and R4 taken together with the carbon and nitrogen atoms to which they are bonded, form a non-aromatic heterocyclic ring optionally fused to an aromatic ring. Preferably R1 and R2 are the same and R3 and R4 are the same. R5-R6 are independently nullH, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. Z is nullO or nullS.
摘要翻译:本发明的一个实施方案是用多药耐药性癌症治疗受试者的方法。 该方法包括向受试者施用有效量的由结构式(I)表示的化合物:Y是共价键或取代或未取代的直链烃基,或Y与两个> C = Z基团一起连接至 其是键合的,是取代或未取代的芳基。 R 1 -R 4独立地为-H,脂族基团,取代的脂族基团,芳基或取代的芳基,或者R 1和R 3与它们所键合的碳原子和氮原子一起,和/或R 2和R 4 与它们所键合的碳原子和氮原子一起形成任选地与芳环稠合的非芳族杂环。 优选地,R 1和R 2相同,并且R 3和R 4相同。 R5-R6独立地是-H,脂族基团,取代的脂族基团,芳基或取代的芳基。 Z = 0或= S。
摘要:
The present invention is directed to compositions and methods for modulating c-Rel-dependent cytokine production without materially altering the level of expression of NFκB and/or the amount of IκB. The present invention is also directed to screening for modulators of c-Rel activity as determined by assaying for altered subcellular localization of c-Rel but where the level of expression of NFκB and/or the amount of IκB is materially unaltered.
摘要:
The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.
摘要:
The present invention is directed to compositions and methods for modulating c-Rel-dependent cytokine production without materially altering the level of expression of NFκB and/or the amount of IκB. The present invention is also directed to screening for modulators of c-Rel activity as determined by assaying for altered subcellular localization of c-Rel but where the level of expression of NFκB and/or the amount of IκB is materially unaltered.