Synthesis and antiproliferative evaluation of novel steroid-benzisoselenazolone hybrids

[Display omitted] •Two novel steroid-benzisoselenazolone hybrids were synthesized.•Hybrids were obtained by condensing of 2-chloroselanylbenzoyl chloride with amino-steroids.•The antiproliferative activity of the hybrids was investigated.•Some hybrids had excellent inhibitory activity on SKOV3 cells...

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Veröffentlicht in:Steroids 2019-12, Vol.152, p.108502-108502, Article 108502
Hauptverfasser: Cui, Jianguo, Wei, Meizhen, Pang, Liping, Gan, Chunfang, Xiao, Junan, Shi, Haixin, Zhan, Junyan, Liu, Zhiping, Huang, Yanmin
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Sprache:eng
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Zusammenfassung:[Display omitted] •Two novel steroid-benzisoselenazolone hybrids were synthesized.•Hybrids were obtained by condensing of 2-chloroselanylbenzoyl chloride with amino-steroids.•The antiproliferative activity of the hybrids was investigated.•Some hybrids had excellent inhibitory activity on SKOV3 cells. The 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 have better inhibitory activity than abiraterone on the proliferation of tumor cells associated with human growth hormone, and have 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.
ISSN:0039-128X
1878-5867
DOI:10.1016/j.steroids.2019.108502