European Journal of Medicinal Chemistry (2021)
Update date:2022-08-10
Topics:
Dong, Jinyun
Huang, Guang
Cui, Qing
Meng, Qingqing
Li, Shaoshun
Cui, Jiahua
Cytochrome P450 1B1 (CYP1B1) has been well validated as an attractive target for cancer prevention and drug resistance reversal. In continuation of our interest in this area, herein, a set of forty-six 6,7,10-trimethoxy-α-naphthoflavone derivatives varying in B ring was synthesized and screened against CYP1 enzymes, leading to the identification of fluorine-containing compound 15i as the most potent and selective CYP1B1 inhibitor (IC50 value of 0.07 nM), being 84-fold more potent than that of the template molecule ANF. Alternatively, the amino-substituted derivative 13h not only possessed a potent inhibitory effect on CYP1B1 (IC50 value of 0.98 nM), but also had a substantially increased water solubility as compared with the lead ANF (311 μg/mL for 13h and <5 μg/mL for ANF). The current study expanded the structural diversity of CYP1B1 inhibitors, and compound 13h could be considered as a promising starting point with great potential for further studies.
View MoreContact:86-791-86629460
Address:1-6F, 118 Xinzhou road, Nanchang, Jiangxi, China
Contact:86-0796-8187704 18507063190
Address:ji'an jiangxi
Compro Shijiazhuang Fine Chemical Co., Ltd
Contact:0086-311-89689838
Address:Economic and Technological Development Zone of Shijiazhuang,Hebei
Shandong General Materials Co.,Ltd(Shandong Aoertong Chemical Co., Ltd)
Contact:86-531-88072280
Address:No. 1825 Hualong Road, Licheng District, Jinan, Shandong, China
Nanjing HuiBaiShi Biotechnology Co.,Ltd.
Contact:+86 (25)58745219
Address:No.606 Ningliu Road,LiuHe District.
Doi:10.1007/s00044-017-1883-0
(2017)Doi:10.1007/BF02540617
(1969)Doi:10.1016/j.jallcom.2013.11.235
(2014)Doi:10.1016/j.apcata.2010.03.050
(2010)Doi:10.1111/j.1551-2916.2009.02923.x
(2009)Doi:10.1002/cmdc.201300263
(2013)