CAS: 154229-19-3; Abiraterone

上下游产品

CAS号154229-18-2 乙酸阿比特龙酯 | CAS号626-55-1 3-溴吡啶 | CAS号34988-34-6 N-[(3-hydroxy-1... | CAS号60-29-7 乙醚 | CAS号32138-69-5 17-碘雄甾-5,16-二烯-... | CAS号89878-14-8 二乙基(3-吡啶基)硼烷 | CAS号53-43-0 去氢表雄酮 | CAS号63015-10-1 雄酮腙 | CAS号154229-18-2 乙酸阿比特龙酯

去氢表雄酮置于2,6-二甲基吡啶,Bis-Triphenylphosphine-Palladium(II) Chloride,碳酸氢钠,Potassium Carbonate,对甲苯磺酸体系中,用 四氢呋喃,甲醇,二氯甲烷,水 用作溶剂,化学反应 58.7H,反应生成阿比特龙
参考文献:基于结构的抑制剂设计,与细胞色素 P450 21A2 相比,对类固醇细胞色素 P450 17A1 的选择性有所提高.
标题:基于结构的抑制剂设计,与细胞色素 P450 21A2 相比,对类固醇细胞色素 P450 17A1 的选择性有所提高.
摘要:抑制雄激素生物合成在临床上可有效治疗雄激素反应性前列腺癌.阿比特龙是雄激素生物合成所需的细胞色素 P450 17A1 (Cyp17A1) 的临床一流抑制剂.然而,阿比特龙也会引起高血压,低钾血症和水肿,部分原因可能是由于另一种类固醇生成细胞色素 P450 Cyp21A2 的脱靶抑制.阿比特龙类似物的设计基于结构证据,即 B 环取代基可能有利地与结合 Cyp17A1 的极性残基相互作用,并与 Cyp21A2 活性位点中的残基发生空间冲突.与阿比特龙的 6.6 倍相比,最好的类似物将 Cyp17A1 抑制的选择性提高了 84 倍.与 Cyp17A1 的共结晶验证了与 Cyp17A1 活性位点残基的预期新接触.将这些类似物对接至 Cyp21A2 中发现了空间冲突,这可能是结合减少和 Cyp21A2 抑制的基础.总体而言,这些类似物可能以减少副作用的形式提供临床优势.
Doi:10.1021/acs.Jmedchem.8B00419

专利信息

专利号:US-12391725-B2
优先权日:2016-06-22
标题:Method for production of novel galeterone analogs and uses thereof
发明人：NJAR VINCENT C O; PURANIK PURUSHOTTAMACHAR; MURIGI FRANCIS
权利人:NJAR VINCENT C O; PURANIK PURUSHOTTAMACHAR; MURIGI FRANCIS; NAT INSTITUTES OF HEALTH NIH U S DEPT OF HEALTH AND HUMAN SERVICES DHHS U S GOVERNMENT
摘要:Galeterone and its C-3 analogs are of substantial interest because of their multi-target anticancer activities, including AR and Mnk degrading activities. Provided are novel procedures for gram-scale, high-yield synthesis of C-3 analogs of galeterone, including 3β-(1H-imidazole-1-yl)-17-(1H-benzimidazole-1-yl)-androsta-5,16-diene (galeterone 3β-imidazole) and 3β-(pyridine-4-ylmethoxy)-17-(1H-benzimidazol-1-yl)androsta-5,16-diene (galeterone 3β-pyridine methoxylate).

专利号:US-11708381-B2
优先权日:2016-11-25
标题:Inhibitors of androgen receptor signaling
发明人：WANG GUANGDI; LIU JIAWANG; ZHENG SHILONG; GUO SHANCHUN
权利人:XAVIER UNIV OF LOUISIANA
摘要:The present disclosure relates to androgen receptor signaling inhibitors and the synthesis of the same. Further, the present disclosure teaches the utilization of the androgen receptor signaling inhibitors in a treatment for proliferative diseases, including cancer, particularly prostate cancer, and especially castration-resistant prostate cancer.

专利号:US-8828984-B2
优先权日:2012-11-19
标题:Gold(III) complexes containing N-heterocyclic carbene ligand, synthesis, and their applications in cancer treatment and thiol detection
发明人：CHE CHI MING; ZOU TAOTAO
权利人:UNIV HONG KONG; UNIV HONG KONG
摘要:Provided herein is a method of synthesis of Au(III)-NHC complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Au(III)-NHC complexes. Also provided is method of detecting thiol in a biological system. The Au(III)-NHC complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, inhibition of thioredoxin reductase activity, and inhibition of tumor growth in vivo.

专利号:US-10577387-B1
优先权日:2018-08-09
标题 :Platinum (II) complexes containing N-heterocyclic carbene ligand and pincer ligands, synthesis, and their applications in cancer treatment
发明人：CHE CHI MING; Fung Sin Ki; Chen tian feng
权利人:UNIV HONG KONG
摘要:Provided herein is a method of synthesis of Pt(II) complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Pt(II) complexes. Also provided is a method of detecting the Pt(II) complex in a biological system. Also provided is a method of making the Pt(II) complex The Pt(II) complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, and inhibition of tumor growth in vivo.

专利号:US-11286271-B2
优先权日:2018-07-31
标 题 :Iridium (III) complexes containing N-heterocyclic carbene ligand, synthesis, and their use thereof in cancer treatment
发明人：CHE CHI MING; LAM TSZ LUNG; TONG KA CHUNG
权利人:UNIV HONG KONG
摘要:Provided herein are Ir(III) complexes comprising N-heterocyclic carbene ligand, method of synthesis of the Ir(III) complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Ir(III) complexes under both dark and light conditions. Also provided is a method of detecting the Ir(III) complex in a biological system. Also provided is a method of making the Ir(III) complex. The Ir(III) complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, and inhibition of tumor growth in vivo.

专利号:US-9884067-B2
优先权日:2013-03-14
标 题:Androgen receptor down-regulating agents and uses thereof
发明人：NJAR VINCENT C O; GEDIYA LALJI K; PURUSHOTTAMACHAR PURANIK; GODBOLE ABHIJIT; KWEGYIR AFFUL ANDREW; VASAITIS TADAS
权利人:UNIV OF MARYLAND EASTERN SHORE; UNIV JEFFERSON; UNIV MARYLAND
摘要:The present disclosure provides the design and synthesis of novel steroidal compounds that cause down-regulation of the androgen receptor (AR), both full length and splice variant. The compounds are potential agents for the treatment of all forms of prostate cancer and other diseases that depend on functional AR.