title: 5α-reductase inhibitors, antiviral and anti-tumor activities of some steroidal cyanopyridinone derivatives.
abstract: We herein report the 5α-reductase inhibitors, antiviral and anti-tumor activities of some synthesized heterocyclic cyanopyridone and cyanothiopyridone derivatives fused with steroidal structure. Initially the acute toxicity of the compounds was assayed via the determination of their LD(50). All the compounds, except 3b, were interestingly less toxic than the reference drug (Prednisolone(®)). Seventeen heterocyclic derivatives containing a cyanopyridone or cyanothiopyridone rings fused to a steroidal moiety were synthesized and screened for their 5α-reductase inhibitors, antiviral and anti-tumor activities comparable to that of Anastrozole, Bicalutamide, Efavirenz, Capravirine, Ribavirin, Oseltamivir and Amantadine as the reference drugs. Some of the compounds exhibited better 5α-reductase inhibitors, antiviral and anti-tumor activities than the reference drugs. The detailed 5α-reductase inhibitors, antiviral and anti-tumor activities of the synthesized compounds were reported.
authors: Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.
authors: Abdullah M
authors: AM
authors: Al-Mohizea
authors: Mohamed A
authors: MA
authors: Al-Omar
authors: Mohamed M
authors: MM
authors: Abdalla
authors: Abdel-Galil E
authors: AG
authors: Amr
mesh_terms: D058891:5-alpha Reductase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D000998:Antiviral Agents / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical / Q000379:methods; D015195:Drug Design; D006367:HeLa Cells; D006801:Humans; D006860:Hydrogen Bonding; D020128:Inhibitory Concentration 50; D008297:Male; D008956:Models, Chemical; D011239:Prednisolone / Q000737:chemistry; D011471:Prostatic Neoplasms / Q000188:drug therapy; D011725:Pyridines / Q000737:chemistry; D051381:Rats; D017207:Rats, Sprague-Dawley; D013256:Steroids / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D058891:5-alpha Reductase Inhibitors; D000970:Antineoplastic Agents; D000998:Antiviral Agents; D011725:Pyridines; D013256:Steroids; D011239:Prednisolone