title: Androgen receptor antagonists and anti-prostate cancer activities of some synthesized steroidal candidates.
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.
authors: Department of Pharmacy, College of Health Science, Taibah University, Madinah 3893, Saudi Arabia.
authors: Saleh Abd El-Rahman
authors: SA
authors: Bahashwan
authors: Mohamed Abd El-Rahman
authors: MA
authors: Al-Omar
authors: Essam
authors: E
authors: Ezzeldin
authors: Mohamed Mostafa
authors: MM
authors: Abdalla
authors: Ahmed Abd El-Hameed
authors: AA
authors: Fayed
authors: Abdel-Galil el-Sayed
authors: AG
authors: Amr
mesh_terms: D059002:Androgen Receptor Antagonists / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D000813:Anilides / Q000633:toxicity; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004354:Drug Screening Assays, Antitumor; D006571:Heterocyclic Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology / Q000633:toxicity; D006801:Humans; D008297:Male; D009570:Nitriles / Q000633:toxicity; D011471:Prostatic Neoplasms; D011944:Receptors, Androgen / Q000737:chemistry / Q000378:metabolism; D013256:Steroids / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D013329:Structure-Activity Relationship; D014105:Tosyl Compounds / Q000633:toxicity
chemical_list: D059002:Androgen Receptor Antagonists; D000813:Anilides; D000970:Antineoplastic Agents; D006571:Heterocyclic Compounds; D009570:Nitriles; D011944:Receptors, Androgen; D013256:Steroids; D014105:Tosyl Compounds; C053541:bicalutamide