Acylpyrogallols as inhibitors of antiapoptotic Bcl-2 proteins.
A series of acylpyrogallols were designed, synthesized, and evaluated as small-molecule inhibitors of antiapoptotic Bcl-2 proteins. The most potent compound 9 (TM-179) binds to Bcl-2 with an IC50 of 170 nM and to Mcl-1 with a Ki of 37 nM. Compound 9 potently inhibits cell growth and induces apoptosis in human breast and prostate cancer cell lines.
Tang
Guozhi
G
Nikolovska-Coleska
Zaneta
Z
Qiu
Su
S
Yang
Chao-Yie
CY
Guo
Jie
J
Wang
Shaomeng
S
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D017209:Apoptosis; D052160:Benzothiazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D008958:Models, Molecular; D019253:Proto-Oncogene Proteins c-bcl-2 / Q000037:antagonists & inhibitors*; D011748:Pyrogallol / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D052160:Benzothiazoles; D019253:Proto-Oncogene Proteins c-bcl-2; C528848:TM 179; D011748:Pyrogallol