CAS: 16372-08-0; 4-Chloro-6,7-Dihydro-5H-Pyrrolo[2,3-D]Pyrimidine

相似化合物

16372-08-0 2139336-89-1 1251761-95-1

[2-(4,6-Dichloro-Pyrimidin-5-yl)-Ethyl]-(4-Methoxy-Benzyl)-Amine置于potassium Phosphate,三氟乙酸体系中,用 二甲基亚砜 用作溶剂,化学反应 16.17H,反应生成4-氯-6,7-二氢-5H-吡咯并[2,3-D]嘧啶
参考文献:1-(2-Hydroxy-2-Methyl-3-Phenoxypropanoyl)Indoline-4-Carbonitrile Derivatives As Potent And Tissue Selective Androgen Receptor Modulators
标题:1-(2-Hydroxy-2-Methyl-3-Phenoxypropanoyl)Indoline-4-Carbonitrile Derivatives As Potent And Tissue Selective Androgen Receptor Modulators
摘要:We Present A Novel Series Of Selective Androgen Receptor Modulators (Sarms) Which Shows Excellent Biological Activity And Physical Properties. 1-(2-Hydroxy-2-Methyl-3-Phenoxypropanoyl)-Indoline-4-Carbonitriles Showed Potent Binding To The Androgen Receptor (Ar) And Activated Ar-Mediated Transcription In Vitro. Representative Compounds Demonstrated Diminished Activity In Promoting The Intramolecular Interaction Between The Ar Carboxyl (C) And Amino (N) Termini. This N/c-Termini Interaction Is A Biomarker Assay For The Undesired Androgenic Responses In Vivo. In Orchidectomized Rats,Daily Administration Of A Lead Compound From This Series Showed Anabolic Activity By Increasing Levator Ani Muscle Weight. Importantly,Minimal Androgenic Effects (Increased Tissue Weights) Were Observed In The Prostate And Seminal Vesicles,Along With Minimal Repression Of Circulating Luteinizing Hormone (Lh) Levels And No Change In The Lipid And Triglyceride Levels. This Lead Compound Completed A Two Week Rat Toxicology Study,And Was Well Tolerated At Doses Up To 100 Mg/kg/day,The Highest Dose Tested,For 14 Consecutive Days.
Doi:10.1021/jm401625B