Improvement in the Anticancer Activity of 6-Mercaptopurine via Combination with Bismuth(III).
6-Mercaptopurine (6-MP) is a clinically important antitumor drug and its commercially available form is provided as monohydrate, belonging to biopharmaceuticals classification system (BCS) class II category. The combination of bismuth(III) (Bi(III)) with 6-MP was proved to significantly improve the anticancer activity of 6-MP, leading to the discovery of a new amorphous complex ([Bi(MP)3(NO3)2]NO3). The prepared [Bi(MP)3(NO3)2]NO3was characterized by the matrix assisted laser desorption-ionization time-of-flight (MALDI-TOF)-MS, etc. Noticeably, according to the in vitro evaluations of cytotoxicity, cellular apoptotic, colony formation as well as cell migration, the anticancer activity of amorphous [Bi(MP)3(NO3)2]NO3was found to be of high therapeutic effect over 6-MP.
University of Shanghai for Science and Technology.
Yang
Y
Yang
Shuang
S
Zhou
Ruizhuo
R
Ouyang
Yaoqin
Y
Yang
Huihong
H
Tao
Kai
K
Feng
Xiaoshen
X
Zhang
Fei
F
Xiong
Ning
N
Guo
Tianyu
T
Zong
Penghui
P
Cao
Yuhao
Y
Li
Yuqing
Y
Miao
D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D017209:Apoptosis / Q000187:drug effects; D002465:Cell Movement / Q000187:drug effects; D049109:Cell Proliferation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D015122:Mercaptopurine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D008968:Molecular Conformation; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D009942:Organometallic Compounds; C037331:bismuth-6-mercaptopurine; D015122:Mercaptopurine