Journal of Medicinal Chemistry p. 5736 - 5748 (2017)
Update date:2022-08-03
Topics:
Ma, Jing
Wang, Qingpeng
Huang, Zhonglv
Yang, Xiande
Nie, Quandeng
Hao, Wenpei
Wang, Peng George
Wang, Xin
Glycosylated platinum(IV) complexes were synthesized as substrates for GLUTs and OCTs for the first time, and the cytotoxicity and detailed mechanism were determined in vitro and in vivo. Galactoside Pt(IV), glucoside Pt(IV), and mannoside Pt(IV) were highly cytotoxic and showed specific cancer-targeting properties in vitro and in vivo. Glycosylated platinum(IV) complexes 5, 6, 7, and 8 (IC50 0.24-3.97 μM) had better antitumor activity of nearly 166-fold higher than the positive controls cisplatin (1a), oxaliplatin (3a), and satraplatin (5a). The presence of a hexadecanoic chain allowed binding with human serum albumin (HSA) for drug delivery, which not only enhanced the stability of the inert platinum(IV) prodrugs but also decreased their reduction by reductants present in human whole blood. Their preferential accumulation in cancer cells compared to noncancerous cells (293T and 3T3 cells) suggested that they were potentially safe for clinical therapeutic use.
View MoreWuhan Soleado Technology Co.,Ltd.
Contact:86-2783341481 18971291927
Address:RM2405 Unit 1 Builing 1, Taiyin Tower, Changqing Road,Wuhan China
GUANGZHOU MEDCAN PHARMATECH LTD
website:http://www.gzmedcan.com
Contact:+86-20-82519649
Address:Building J,Room 101,1 JiangtashanRd,Guang Zhou Science City,Guang Zhou ,China
Contact:86-21 60347964
Address:No.1304, West Meilong Road, Minhang District, Shanghai, China
SHIJIAZHUANG CHENSHI IMPORT AND EXPORT CO.,LTD
Contact:+86-311-89871056
Address:RM2017 BUILDING CTIANSHAN GALAXY PLAZA,NO168 CHANGJIANG ROAD,GAOXIN DISTRICT,SHIJIAZHUANG CITY, HEBEI,CHINA
Shandong LuZhou Amino Acid Co., Ltd
Contact:86-539-2218025
Address:yishui economic and technical development zone zhenxing south road
Doi:10.1016/S0031-9422(00)83049-6
(1985)Doi:10.1248/cpb.11.1271
(1963)Doi:10.1016/S0040-4020(01)98391-7
(1964)Doi:10.1016/S0040-4020(01)98809-X
(1984)Doi:10.3390/molecules26103033
(2021)Doi:10.1039/j39700000513
(1970)