An efficient and general approach for the synthesis of amphiphilic 1,2-amino alcohols is reported. The use of N-benzyl protecting groups is essential for obtaining good yields when opening a long-chain terminal epoxide with an amine.
The present invention comprises small molecular weight, non-peptidic inhibitors of formulae I-VII of Protein Tyrosine Phosphatase 1 (PTP1) which are useful for the treatment and/or prevention of Non-Insulin Dependent Diabetes Mellitus (NIDDM).
[(1-Pyrenylmethyl)amino] alcohols, a new class of antitumor DNA intercalators. Discovery and initial amine side chain structure-activity studies
作者:Kenneth W. Bair、Richard L. Tuttle、Vincent C. Knick、Michael Cory、David D. McKee
DOI:10.1021/jm00171a012
日期:1990.9
additional basic amine groups in the sidechain enhances DNA binding due to electrostatic interactions. Those compounds containing only a single basic benzylic amine bind similarly to DNA. Only the presence of bulky sidechains appears to decrease the DNA interactions in the compounds examined. Although antitumor activity is seen for (1-pyrenylmethyl)amino alcohols, useful antitumor activity in the series
Fluorescence Polarization for the Evaluation of Small-Molecule Inhibitors of PCAF BRD/Tat-AcK50 Association
作者:Ping Hu、Xinghui Wang、Baiqun Zhang、Shuai Zhang、Qiang Wang、Zhiyong Wang
DOI:10.1002/cmdc.201300499
日期:2014.5
efficiently screen and evaluate inhibitors of PCAF bromodomain/Tat‐AcK50 protein–peptide interaction. A series of pyridine 1‐oxide derivatives were synthesized and evaluated. Some of the novel compounds, 2‐(3‐aminopropylamino) pyridine 1‐oxide derivatives, could be effective inhibitors of PCAF bromodomain/Tat‐AcK50 association. Specifically, 2‐(3‐aminopropylamino)‐5‐(hydroxymethyl)pyridine 1‐oxide hydrochloride
This disclosure describes platinum chelates of 2-hydrazino-1-aza (or 1,3-diaza,1-oxa-3-aza or 1-thia-3-aza)-1-cyclo-alkenes which possess activity as antitumor agents.