通过生物正交化学反应在活细胞中激活的 O-衍生的重氮二羟酸盐的合成与评价。
Synthesis and Evaluation of O-Derived Diazeniumdiolates Activatable via Bioorthogonal Chemistry Reactions in Living Cells.
机构信息
State Key Laboratory of Natural Medicines, Jiangsu Key Laboratory of Drug Discovery for Metabolic Diseases, Jiangsu Key Laboratory of Drug Screening , China Pharmaceutical University , Nanjing 210009 , P. R. China.
State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences , University of Macau , Macao , China.
出版信息
Org Lett. 2018 Apr 20;20(8):2164-2167. doi: 10.1021/acs.orglett.8b00423. Epub 2018 Mar 29.
A class of O-alkyl derived diazeniumdiolates 3a-f and 4a-c were designed and synthesized as new bioorthogonal NO precursors, which can be effectively uncaged in the presence of a palladium catalyst via bioorthogonal bond cleavage reactions to generate NO in living cancer cells, eliciting potent antiproliferative activity.
一类 O-烷基取代的重氮烷二酸盐 3a-f 和 4a-c 被设计并合成作为新型生物正交的 NO 前体，在钯催化剂的存在下通过生物正交键断裂反应可以有效地释放出 NO ，从而在活的癌细胞中产生强烈的抗增殖活性。
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