CAS: 2011-70-3; N-(2-Benzoyl-4-Nitrophenyl)-2-Bromoacetamide

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CAS号598-21-0 溴乙酰溴 | CAS号1775-95-7 2-氨基-5-硝基二苯酮 | CAS号100-01-6 对硝基苯胺 | CAS号98-88-4 苯甲酰氯 | CAS号2011-69-0 2-amino-N-(2-be... | CAS号24143-26-8 10-nitro-11b-ph...

📜4-硝基苯胺置于zinc(II) Chloride体系中,用 甲苯 用作溶剂,化学反应 0.03H,反应生成5-硝基-2-(溴乙酰氨基)二苯甲酮
参考文献:含氮芥子基部分作为潜在中枢神经系统抗肿瘤剂的氨基二苯甲酮衍生物的设计,合成和评估
标题:含氮芥子基部分作为潜在中枢神经系统抗肿瘤剂的氨基二苯甲酮衍生物的设计,合成和评估
摘要:合成了一系列含有氮芥子部分(5A-F)的新型取代氨基二苯甲酮衍生物,并根据其ir,1 H NMR,13 C NMR,Chn和质谱数据进行了表征.当评估4-(4-硝基苄基)吡啶烷基化化学活性时,所有化合物均证明是活性烷基化剂.通过计算,在线软件和qikprop 3.2对所有合成的化合物进行中枢神经系统(cns)活动所需的理化参数测定.日志p值和分析的其他计算机模拟adme理化指标位于非常好bbb渗透所需的范围之间.对人癌细胞系的体外抗增殖活性.研究了549(肺),Colo 205(结肠),U 87(胶质母细胞瘤)和imr-32(神经母细胞瘤).大多数测试化合物显示出有效的抗肿瘤活性,尤其是化合物(5F)显示出最高的抗cns癌细胞活性,与苯丁酸氮芥和多西紫杉醇相当.初步的构效关系(sar)表明,5-氯氨基二苯甲酮-芥末系列(5A-C)比5-硝基氨基二苯甲酮-芥末系列(5D-F)表现出更好的抗肿瘤活性.
Doi:10.1007/s00044-013-0582-8

专利信息

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:RU-2136285-C1
优先权日:1996-04-23
标题:Method of synthesis of drug nitrazepam - 1,3-dihydro-5-phenyl-7-nitro-2h-1,4-benzodiazepine-2-one