Novel class of cytodifferentiating agents and histone deacetylase inhibitors, and methods of use thereof
申请人:Breslow Ronald
公开号:US20070010536A1
公开(公告)日:2007-01-11
The present invention provides the compound having the formula:
wherein each of R
1
and R
2
is, substituted or unsubstituted, aryl, cycloalkyl, cycloalkylamino, naphtha, pyridineamino, piperidino, t-butyl, aryloxy, arylalkyloxy, or pyridine group; wherein A is an amido moiety, —O—, —S—, —NH—, or —CH
2
—; and wherein n is an integer from 3 to 8. The present invention also provides a method of selectively inducing growth arrest, terminal differentiation and/or apoptosis of neoplastic cells and thereby inhibiting proliferation of such cells. Moreover, the present invention provides a method of treating a patient having a tumor characterized by proliferation of neoplastic cells. Lastly, the present invention provides a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically acceptable amount of the compound above.
本发明提供了具有以下式子的化合物:其中R1和R2分别为取代或未取代的芳基、环烷基、环烷基氨基、萘基、吡啶氨基、哌啶基、叔丁基、芳氧基、芳基烷氧基或吡啶基;其中A为酰胺基、-O-、-S-、-NH-或-CH2-;n为3到8的整数。本发明还提供了一种选择性诱导肿瘤细胞生长停滞、终末分化和/或凋亡的方法,从而抑制这些细胞的增殖。此外,本发明还提供了一种治疗具有肿瘤细胞增殖特征的患者的方法。最后,本发明提供了一种包括药学上可接受的载体和上述化合物的治疗上可接受的剂量的药物组合物。