Hector F. DeLuca;Katarzyna Sokolowska;Lori A. Plum;Margaret Clagett-Dame;Rafal R. Sicinski;Antonio Mouriño
发明人:
Hector F. DeLuca,Katarzyna Sokolowska,Lori A. Plum,Margaret Clagett-Dame,Rafal R. Sicinski,Antonio Mouriño
申请号：
US12895577
公开号：
US08178517B2
申请日:
2010.09.30
申请国别(地区):
US
年份:
2012
代理人:
摘要：
This invention discloses 6-methylvitamin D3 analogs, and specifically 1α,25-dihydroxy-6-methylvitamin D3, and pharmaceutical uses therefor. This compound exhibits vitamin D receptor binding activity and transcription activity as well as activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as an anti-cancer agent, especially for the treatment or prevention of leukemia, colon cancer, breast cancer, skin cancer or prostate cancer. This compound also exhibits low in vivo calcemic activity, but because it binds the receptor with the same affinity as the native hormone calcitriol, it may act as an antagonist to inhibit development of hypercalcemia.
