CAS: 199850-67-4; (S)-2-(4'-Bromo-[1,1'-Biphenyl]-4-Ylsulfonamido)-3-Methylbutanoic Acid

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CAS号92-66-0 4-溴联苯 | CAS号13610-11-2 4′-溴代联苯-4-磺酰氯 | CAS号78079-08-0 4-溴-4-硫联苯

📜4-溴代联苯置于氯磺酸,氯化亚砜,苯甲醚,三乙胺,三氟乙酸体系中,用 四氢呋喃,氯仿,水,N,N-二甲基甲酰胺 用作溶剂,化学反应 15.75H,反应生成(S)-2-(4'-溴联苯-4-磺酰胺)-3-甲基丁酸
参考文献:一系列有效的,系统可用的联苯磺酰胺基质金属蛋白酶抑制剂的结构活性关系和药代动力学分析.
标题:一系列有效的,系统可用的联苯磺酰胺基质金属蛋白酶抑制剂的结构活性关系和药代动力学分析.
摘要:制备了一系列(S)-2-(联苯基-4-磺酰基氨基)-3-甲基丁酸(5)的联苯磺酰胺衍生物,并评估了它们抑制基质金属蛋白酶(mmps)的能力.对于这一系列化合物,我们的目标是用结构上不同的功能性系统取代取代基上5的联苯和α-位置的取代基,以评估这些变化对生物学和药代动力学活性的影响.随后的结构活性关系(sar)研究表明,在4'-位(11C)处被溴取代的联苯磺酰胺显着提高了体外活性,并显示出优异的药代动力学(c(max),T(1/2),Aucs,相对于化合物5而言,可以通过用各种取代基取代11C的异丙基来改变α位的亲脂性,一般而言,与mmp-2,-3和-13相比,药效保持不变,但口服系统利用率较低.随后对其对映异构体11C'的评估表明,两种化合物都是同等有效的mmp抑制剂.相反,相应的异羟肟酸对映体对16A(s-异构体)和16A'(r-异构体)立体选择性抑制了mmp.在该系列中,16A'首次提
Doi:10.1021/jm9903141

专利信息

专利号:US-11285169-B2
优先权日:2013-03-13
标题 :Methods for modulating chemotherapeutic cytotoxicity
发明人：ROBERTS DAVID D; SOTO PANTOJA DAVID R
权利人:US HEALTH
摘要:Methods of reducing cytotoxicity of a chemotherapeutic agent to non-cancer cells by administering to a subject with cancer an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent, such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are provided. Example disclosed methods reduce cardiotoxicity. In one example, the methods include administering to a subject with cancer an effective amount of a CD47 antisense morpholino oligonucleotide and an anthracycline such as doxorubicin. Methods of increasing cytotoxicity of a chemotherapeutic agent in cancer cells by administering to a subject with a tumor an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are also provided. In some embodiments, the inhibitor of CD47 signaling is administered to the subject before, during, or after the administration of the DNA damaging agent.