5α-Reductase inhibitors, antiviral and anti-tumor activities of some steroidal cyanopyridinone derivatives

Al-Mohizea A.M.; Al-Omar M.A.; Abdalla M.M.; Amr A.G.E.

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5α-Reductase inhibitors, antiviral and anti-tumor activities of some steroidal cyanopyridinone derivatives

机译：5α-还原酶抑制剂，某些甾体氰基吡啶并酮衍生物的抗病毒和抗肿瘤活性

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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.

机译：我们在此报告了5α-还原酶抑制剂，一些合成的与甾体结构融合的杂环氰基吡啶酮和氰基硫代吡啶酮衍生物的抗病毒和抗肿瘤活性。最初，通过确定其LD_（50）来测定化合物的急性毒性。有趣的是，除3b外，所有化合物的毒性均低于参考药物（泼尼松龙〜？）。合成了十七个含有与甾体部分稠合的氰基吡啶酮或氰基硫吡啶酮环的杂环衍生物，并筛选了与阿那曲唑，比卡鲁胺，依法韦伦，Capravirine，利巴韦林，奥瑟他米韦和金刚烷胺为同等作用的5α-还原酶抑制剂，抗病毒和抗肿瘤活性。参考药物。与参考药物相比，某些化合物具有更好的5α-还原酶抑制剂，抗病毒和抗肿瘤活性。报道了合成化合物的详细5α-还原酶抑制剂，抗病毒和抗肿瘤活性。

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《International Journal of Biological Macromolecules: Structure, Function and Interactions》 |2012年第1期|共9页
作者
Al-Mohizea A.M.; Al-Omar M.A.; Abdalla M.M.; Amr A.G.E.;
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正文语种 eng
中图分类生物大分子的结构和功能;
关键词
5α-Reductase inhibitors; Antiviral and anti-tumor activities; Cyanopyridones; Cyanothiopyridones; Steroid;

机译：5α-还原酶抑制剂;抗病毒和抗肿瘤活性;氰基吡啶酮;氰基硫吡啶酮;类固醇;

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1. 5α-Reductase inhibitors, antiviral and anti-tumor activities of some steroidal cyanopyridinone derivatives [J] . Al-Mohizea A.M., Al-Omar M.A., Abdalla M.M., International Journal of Biological Macromolecules: Structure, Function and Interactions . 2012,第1期

机译：5α-还原酶抑制剂，某些甾体氰基吡啶并酮衍生物的抗病毒和抗肿瘤活性
2. Synthesis and biological evaluation of 4-(4-(alkyl- and phenylaminocarbonyl)benzoyl)benzoic acid derivatives as non-steroidal inhibitors of steroid 5 alpha-reductase isozymes 1 and 2. [J] . Salem OI, Schulz T, Hartmann RW Archiv der Pharmazie . 2002,第2a3期

机译：4-（4-（烷基-和苯氨基羰基）苯甲酰基）苯甲酸衍生物作为甾体5α-还原酶同工酶1和2的非甾体抑制剂的合成及生物学评估。
3. SYNTHESIS OF PHENANTHRIDIN-3-ONE DERIVATIVES - NON-STEROIDAL INHIBITORS OF STEROID 5-ALPHA-REDUCTASE [J] . Mook RA., Bennett C., Lackey K. Tetrahedron letters: The International Journal for the Rapid Publication of Preliminary Communications in Organic Chemistry . 1995,第23期

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6. Identification of danthron as an isoform-specific inhibitor of HEME OXYGENASE-1/cytochrome P450 reductase interaction with anti-tumor activity [O] . Yi-Tai Chou, Fu-Fei Hsu, Dun-Yao Hu, 2018

机译：丹当隆是一种具有抗肿瘤活性的HEME OXYGENASE-1 /细胞色素P450还原酶相互作用的同工型特异性抑制剂
7. Design, synthesis and structure-activity relationships studies on steroidal aromatase and 5α-reductase inhibitors as anti-tumors [O] . Varela Carla 2013

机译：类固醇芳香酶和5α-还原酶抑制剂作为抗肿瘤药物的设计，合成及构效关系研究

5α-Reductase inhibitors, antiviral and anti-tumor activities of some steroidal cyanopyridinone derivatives

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