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Titanocene(III) chloride-mediated reductions of oxazines, hydroxamic acids, and N-hydroxy carbamates.二氯二茂钛（III）介导的恶嗪、异羟肟酸和N-羟基氨基甲酸酯的还原反应。
J Org Chem. 2009 Jan 2;74(1):448-51. doi: 10.1021/jo802184y.
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Novel 1,4-benzodiazepine derivatives with antiproliferative properties on tumor cell lines.对肿瘤细胞系具有抗增殖特性的新型1,4 - 苯二氮䓬衍生物。
Bioorg Med Chem Lett. 2007 May 1;17(9):2527-30. doi: 10.1016/j.bmcl.2007.02.016. Epub 2007 Feb 9.
3
The immunomodulatory benzodiazepine Bz-423 inhibits B-cell proliferation by targeting c-myc protein for rapid and specific degradation.免疫调节性苯二氮䓬类药物Bz - 423通过靶向c - myc蛋白进行快速特异性降解来抑制B细胞增殖。
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Oxazoline N-oxide-mediated [2+3] cycloadditions. Application to a synthesis of (-)-tetrahydrolipstatin.恶唑啉氮氧化物介导的[2+3]环加成反应。应用于（-）-四氢脂抑素的合成。
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Protein farnesyltransferase inhibitors exhibit potent antimalarial activity.蛋白质法尼基转移酶抑制剂具有强大的抗疟活性。
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Chemoenzymatic synthesis and synthetic application of enantiopure aminocyclopentenols: total synthesis of carbocyclic (+)-uracil polyoxin C and its alpha-epimer.对映体纯氨基环戊烯醇的化学酶法合成及其合成应用：碳环（+）-尿嘧啶多氧霉素C及其α-差向异构体的全合成
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Crystal structures of the anticancer clinical candidates R115777 (Tipifarnib) and BMS-214662 complexed with protein farnesyltransferase suggest a mechanism of FTI selectivity.与蛋白法尼基转移酶复合的抗癌临床候选药物R115777（替匹法尼）和BMS - 214662的晶体结构揭示了法尼基转移酶抑制剂（FTI）选择性的机制。
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新型含异羟肟酸的1,4-苯二氮䓬类化合物的合成及其抗癌活性

Synthesis and anticancer activity of new hydroxamic acid containing 1,4-benzodiazepines.

作者信息

Tardibono Lawrence P, Miller Marvin J

机构信息

Department of Chemistry and Biochemistry, University of Notre Dame, Notre Dame, Indiana 46556, USA.

出版信息

Org Lett. 2009 Apr 2;11(7):1575-8. doi: 10.1021/ol900210h.

DOI:10.1021/ol900210h
PMID:19320504
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2725444/
Abstract

By employing an intramolecular Pd(0)-mediated ring opening of an acylnitroso-derived cycloadduct, new hydroxamic acid containing benzodiazepines have been synthesized and have demonstrated biological activity in MCF-7 and PC-3 tumor cell lines. Subsequent N-O bond reduction of the hydroxamate has provided access to amide analogues for SAR studies. During the course of our syntheses, an intermediate oxazoline N-oxide was isolated and gave insight into the mechanism of the key Pd(0)-mediated reaction.

摘要

通过利用分子内钯（0）介导的酰基亚硝基衍生的环加成物的开环反应，合成了含异羟肟酸的新型苯二氮䓬类化合物，并在MCF-7和PC-3肿瘤细胞系中显示出生物活性。随后对异羟肟酸进行N-O键还原，得到酰胺类似物用于构效关系研究。在我们的合成过程中，分离出一种中间体恶唑啉N-氧化物，并深入了解了关键的钯（0）介导反应的机理。