Abd El-Galil E. Amr,Mohamed A. Al-Omar,Abdulrahman A. Almehizia
申请号:
US15897912
公开号:
US10064837B1
申请日:
2018.02.15
申请国别(地区):
US
年份:
2018
代理人:
摘要:
The abietic acid derivatives as anti-tumor agents are derivatives of abietic acid in which the hydroxyl entity (—OH) of the carboxyl entity is replaced by an electronegative substituent, which may be C6H5-O—, C6H5-S—, or C6H5-NH—, and a hydrogen atom on one of the rings is replaced by a hydroxyl (—OH) substituents, the derivatives having the formula:wherein X is O, S, or NH. The derivatives are formed by formation of an intermediate lactone from abietic acid, followed by reaction of the lactone with phenol, thiophenol, or aniline. All of the derivatives exhibited potent 5α-reductase inhibitor activity, both in vitro and in vivo, and anti-tumor activity with regard to two prostate cancer cell lines—LNCaP and PC-3. The intermediate lactones are also derivatives of abietic acid that exhibit anti-tumor activity.