Androgen receptor antagonists and anti-prostate cancer activities of some synthesized steroidal candidates |
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Authors: | Bahashwan Saleh Abd El-Rahman Al-Omar Mohamed Abd El-Rahman Ezzeldin Essam Abdalla Mohamed Mostafa Fayed Ahmed Abd El-Hameed Amr Abdel-Galil el-Sayed |
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Affiliation: | Department of Pharmacy, College of Health Science, Taibah University, Madinah 3893, Saudi Arabia. |
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Abstract: | In continuation of our previous work, a novel series of steroid derivatives were synthesized and their androgen receptor (AR) antagonist activities and in vivo antiandrogenic properties were evaluated. Twenty-one heterocyclic derivatives containing a cyanopyrane ring fused to a steroidal moiety were conveniently synthesized and screened for their antagonistic, antiandrogen and prostate anticancer activities comparable to that of bicalutamide as the reference control. Some of the compounds exhibited better antagonistic, antiandrogen and prostate anticancer activities than the reference controls. Initially the acute toxicity of the compounds was assayed via the determination of their LD(50). Synthetic steroidal structures fused to a substituted cyanopyrane ring seem to be a promising approach in the search for novel leads for potent antagonistic, antiandrogen and prostate anticancer agents. |
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