📜4-氯-3-硝基苯甲酸置于4-二甲氨基吡啶,10 Wt% Pd(Oh)2 On Carbon,氢气,Potassium Carbonate,N,N'-二环己基碳二亚胺体系中,用 甲醇,二氯甲烷,水,二甲基亚砜 用作溶剂,化学反应 52.0H,反应生成3-氨基-4-环己基氨基苯甲酸乙酯 参考文献:Novel Arylalkylamine Compounds Exhibits Potent Selective Antiparasitic Activity Against Leishmania Major 标题:Novel Arylalkylamine Compounds Exhibits Potent Selective Antiparasitic Activity Against Leishmania Major 摘要:Leishmania Major (L. Major) Is A Protozoan Parasite Causal Agent Of Leishmaniasis. It Is Estimated That 12 Million People Are Currently Infected And Around 2 Million Infections occur Each Year. Current Treatments Suffer Of High Toxicity For The Patient,Low Efficacy Toward The Parasite,High Cost,And Are Losing Effectiveness Due To Parasite Resistance. Discovering Novel Small Molecule With High Specificity/selectivity And Drug-Like Properties For Anti-Leishmanial Activity Remains A Significant Challenge. The Purpose Of This Study Is To Communicate The Design And Synthesis Strategies Of Novel Chemical Compounds Based Of The Arylalkylamine Scaffold With Selective Toxicity Towards L. Major And Less Toxicity To Human Cells In Vitro. Here,We Have Developed A Structure Activity Relationship (Sar) Study Of Arylalkylamine Aa1 In Order To Study Their Anti-Parasitic Effect In L. Major. Overall,27 Arylalkylamine Compounds Derived From Aa1 Were Synthesized And Purified By Silica Gel Column Chromatography. The Purity Of Each Analog Was Confirmed By Spectroscopic Methods (H-1,C-13 NMR And Lc/ms). Among These Analogs,The Compound Aa9 Showed The Best Toxic Activity On L. Major (Ld50 = 3.34 Mu M),Which Represents A 9 Fold Higher Lethality As Compared With Its Parental Aa1 (Fer-1) Compound (Ld50 = 28.75 Mu M). In Addition,Aa9 Showed No Significant Toxicity At 80 Mu M On U20S Human Osteoblasts,Raw 264.7 Macrophages Or Intraperitoneal Macrophages. In Summary,Our Combined Sar Study And Biological Evaluation Data Of Aa1-Aa27 Compounds Allow The Identification Of Novel Arylalkylamine Compound Aa9 That Exhibits Potent Cytotoxicity Against L. Major Promastigote With Minimum Toxic Effect On Human Cells. (C) 2015 Elsevier Ltd. All Rights Reserved. Doi:10.1016/j.Bmcl.2015.09.041
专利号:US-2025099407-A1 优先权日:2023-09-22 标题:2-amino benzophenone derivatives for targeted ferroptosis induction in cancer therapy 发明人:ALLIMUTHU DHARMARAJA; YADAV DHARMENDRA K; TIWARI SONA; KHANNA SHWETA; VECHALAPU SAI KUMARI 权利人:INDIAN INSTITUTE OF TECH KANPUR 摘要:The present invention discloses a novel class of covalent small molecules comprising 2-amino benzophenone derivatives for targeted ferroptosis induction in cancer cells. The present invention also includes strategies for target identification, hit-to-lead optimization, and combination therapies to enhance therapeutic efficacy. A synthesis and characterization of a library of unique organic structural scaffolds encompassing natural/unnatural amino acids, aromatic and heterocyclic linkers coupled with electrophilic units possessing diverse nucleophile reactivity profiles is provided. The molecules exhibit sub-micromolar to nanomolar inhibitory potency (IC 50 ) when screened against a panel of cancer cell lines including MCF7 (breast cancer), MDA-MB-231 (triple negative breast cancer), 22Rv1 (Prostate), PC3, (prostate cancer), Jurkat J6 (acute T-cell Leukaemia), RPMI 8226 (B lymphocytes), U87MG (glioblastoma), HCT-116 (colon cancer) and A375 (melanoma)) and kidney cells (HEK293). The molecules exhibit potent antiproliferative effects across various cancer cell lines, offering a promising alternative to conventional chemotherapies with reduced side effects.
专利号:US-2025281509-A1 优先权日:2021-04-26 标 题 :Sequential hormone therapy to improve survival and enhance response to immune therapy in men with prostate cancer 发明人:DENMEADE SAMUEL R; ISAACS JOHN T; ANTONARAKIS EMMANUEL S; KACHHAP SUSHANT; MARKOWSKI MARK CHRISTOPHER 权利人:UNIV JOHNS HOPKINS 摘要:Disclosed are methods for treating men with castrate resistant prostate cancer with a sufficient dose of testosterone to achieve supraphysiologic serum levels of testosterone in sequence with androgen ablative treatment or androgen synthesis inhibitors for one or more cycles until evidence of radiographic progression, at which point the subject will receive immune checkpoint blockade therapy.
专利号:CN-117959430-A 优先权日:2023-11-13 标题:Use of inhibiting 7-dehydrocholesterol synthesis in the treatment of tumors
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合成参考文献
参考文献:10.1016/j.canlet.2018.04.021 摘要:Wang Z, Ding Y, Wang X, Lu S, Wang C, He C, Wang L, Piao M, Chi G, Luo Y, Ge P. Pseudolaric acid B triggers ferroptosis in glioma cells via activation of Nox4 and inhibition of xCT. Cancer Lett. 2018 Aug 01;428():21–33. doi: 10.1016/j.canlet.2018.04.021. 参考文献:10.1016/j.toxlet.2021.07.010 摘要:Jian B, Pang J, Xiong H, Zhang W, Zhan T, Su Z, Lin H, Zhang H, He W, Zheng Y. Autophagy-dependent ferroptosis contributes to cisplatin-induced hearing loss. Toxicol Lett. 2021 Oct 10;350():249–60. doi: 10.1016/j.toxlet.2021.07.010. 参考文献:10.1002/path.5882 摘要:Martín‐Saiz L, Guerrero‐Mauvecin J, Martín‐Sanchez D, Fresnedo O, Gómez MJ, Carrasco S, Cannata‐Ortiz P, Ortiz A, Fernandez JA, Sanz AB. Ferrostatin‐1 modulates dysregulated kidney lipids in acute kidney injury. The Journal of Pathology. 2022 Mar 23;257(3):285–99. doi: 10.1002/path.5882.