Synthesis and Antiproliferative Evaluation of Novel Steroid-Benzisoselenazolone Hybrids

Publication date: Available online 20 September 2019Source: SteroidsAuthor(s): Jianguo Cui, Meizhen Wei, Liping Pang, Chunfang Gan, Junan Xiao, Haixin Shi, Junyan Zhan, Zhiping Liu, Yanmin HuangAbstractThe two different types of steroidal benzisoselenazolone hybrids were synthesized by incorporating benzisoselenazolone scaffold into dehydroepiandrosterone and B-norcholesterol. The antiproliferative activity of the synthesized compounds against some carcinoma cell lines were investigated. The results showed that some of these compounds had better inhibitory activity than abiraterone on the proliferation of tumor cells associated with human growth hormone, and had less cytotoxicity on normal human cells. In particular, the IC50 values of the compound 8a and 8f are 5.4 and 6.5 µmol/L against human ovarian carcinoma (SKOV3) cell line, and possess SI values of 13.9 and 10.5, respectively. The information obtained from the studies may be useful for the design of novel chemotherapeutic drugs.Graphical abstract
Source: Steroids - Category: Drugs & Pharmacology Source Type: research