A Novel Oral Selective Estrogen Receptor Down-regulator, AZD9496, drives Tumour Growth Inhibition in Estrogen Receptor positive and ESR1 Mutant Models

A Novel Oral Selective Estrogen Receptor Down-regulator, AZD9496, drives Tumour Growth Inhibition in Estrogen Receptor positive and ESR1 Mutant Models Descriptor: (E)-3-(3,5-DIFLUORO-4-((1R,3R)-2-(2-FLUORO-2- METHYLPROPYL)-3-METHYL-2,3,4,9-TETRAHYDRO-1H-PYRIDO(3,4-B)INDOL-1-YL)PHENYL)ACRYLIC ACID, ESTROGEN RECEPTOR Authors: Norman, R.A, Weir, H.M, Bradbury, R.H, Lawson, M, Rabow, A.A, Buttar, D, Callis, R.J, Curwen, J.O, de Almeida, C, Ballard, P, Hulse, M, Donald, C.S, Feron, L.J.L, Gingell, H, Karoutchi, G, MacFaul, P, Moss, T, Pearson, S.E, Tonge, M, Davies, G, Walker, G.E, Wilson, Z, Rowlinson, R, Powell, S, Hemsley, P, Linney, E, Campbell, H, Ghazoui, Z, Sadler, C, Richmond, G, Pazolli, E, Mazzola, A.M, DCruz, C, De Savi, C. Deposit date: 2015-08-15 Release date: 2015-12-16 Last modified: 2024-05-01 Method: X-RAY DIFFRACTION (1.88 Å) Cite: Optimization of a Novel Binding Motif to (E)-3-(3,5-Difluoro-4-((1R,3R)-2-(2-Fluoro-2-Methylpropyl)-3-Methyl-2, 3,4,9-Tetrahydro-1H-Pyrido[3,4-B]Indol-1-Yl)Phenyl)Acrylic Acid (Azd9496), a Potent and Orally Bioavailable Selective Estrogen Receptor Downregulator and Antagonist. J.Med.Chem., 58, 2015

新型口服选择性雌激素受体降解剂（Selective Estrogen Receptor Down-regulator）AZD9496，可在雌激素受体阳性及ESR1突变模型中诱导肿瘤生长抑制。
描述符：(E)-3-(3,5-二氟-4-((1R,3R)-2-(2-氟-2-甲基丙基)-3-甲基-2,3,4,9-四氢-1H-吡啶并[3,4-b]吲哚-1-基)苯基)丙烯酸，雌激素受体
作者：Norman, R.A.、Weir, H.M.、Bradbury, R.H.、Lawson, M.、Rabow, A.A.、Buttar, D.、Callis, R.J.、Curwen, J.O.、de Almeida, C.、Ballard, P.、Hulse, M.、Donald, C.S.、Feron, L.J.L.、Gingell, H.、Karoutchi, G.、MacFaul, P.、Moss, T.、Pearson, S.E.、Tonge, M.、Davies, G.、Walker, G.E.、Wilson, Z.、Rowlinson, R.、Powell, S.、Hemsley, P.、Linney, E.、Campbell, H.、Ghazoui, Z.、Sadler, C.、Richmond, G.、Pazolli, E.、Mazzola, A.M.、DCruz, C.、De Savi, C.
提交日期：2015年8月15日
发布日期：2015年12月16日
最后修改日期：2024年5月1日
检测方法：X射线衍射（1.88 Å）
引用文献：《针对强效口服生物可利用选择性雌激素受体降解剂与拮抗剂AZD9496（即(E)-3-(3,5-二氟-4-((1R,3R)-2-(2-氟-2-甲基丙基)-3-甲基-2,3,4,9-四氢-1H-吡啶并[3,4-b]吲哚-1-基)苯基)丙烯酸）的新型结合基序优化》，《药物化学杂志》，2015年，第58卷。