Provided herein, inter alia, are methods and compounds for targeted autophagy.
本文提供了针对靶向自噬的方法和化合物。
Parthenolide Covalently Targets and Inhibits Focal Adhesion Kinase in Breast Cancer Cells
作者:Charles A. Berdan、Raymond Ho、Haley S. Lehtola、Milton To、Xirui Hu、Tucker R. Huffman、Yana Petri、Chad R. Altobelli、Sasha G. Demeulenaere、James A. Olzmann、Thomas J. Maimone、Daniel K. Nomura
DOI:10.1016/j.chembiol.2019.03.016
日期:2019.7
parthenolide in human breast cancer cells. We find that parthenolide, as well as other related exocyclic methylene lactone-containing sesquiterpenes, covalently modify cysteine 427 of focal adhesion kinase 1 (FAK1), leading to impairment of FAK1-dependent signaling pathways and breast cancer cell proliferation, survival, and motility. These studies reveal a functional target exploited by members of a
Enhanced Nucleophilicity of <i>N</i>-Aryl Amides with peri-CH and Their Condensations with Formaldehyde
作者:Chunbao Li、Qiang Wang、Xiaoxue Cui、Shasha Liu、Lili Sun
DOI:10.1055/s-2008-1078485
日期:——
N-Aryl amides with peri-CH are capable to condense with formaldehyde to yield N-hydroxymethylated N-aryl amides. The enhanced nucleophilicity is attributed to the single conjugation of the amide nitrogen with the acyl group but not the aryl group. Infrared measurements provide additional evidence for the enhanced nucleophilicity of the amides with peri-CH.
The present invention discloses compounds of formulae (I) and (II) or pharmaceutically acceptable salts, esters, or prodrugs thereof:
which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.
Disulfide Promoted C−P Bond Cleavage of Phosphoramide: “P” Surrogates to Synthesize Phosphonates and Phosphinates
作者:Fei Hou、Xing‐Peng Du、Anwar I. Alduma、Zhi‐Feng Li、Cong‐De Huo、Xi‐Cun Wang、Xiao‐Feng Wu、Zheng‐Jun Quan
DOI:10.1002/adsc.202000511
日期:2020.11.4
A metal‐free C−P bond cleavage reaction is described herein. Phosphoramides, a phosphine source, can react with alcohols to produce phosphonate and phosphinate derivatives in the presence of a disulfide. P−H2, P‐alkyl, and P,P‐dialkyl phosphoramides can be used as substrates to obtain the corresponding pentavalent phosphine products.
本文描述了无金属的C-P键裂解反应。磷酰胺(一种膦源)可以在二硫化物存在下与醇反应生成膦酸酯和次膦酸酯衍生物。P H 2,P-烷基和P,P-二烷基磷酰胺可用作底物,以获得相应的五价膦产品。