Tian, Zong-Qiang published the artcileSynthesis and biological activities of novel 17-aminogeldanamycin derivatives, Safety of 2-(Azetidin-1-yl)ethanamine, the publication is Bioorganic & Medicinal Chemistry (2004), 12(20), 5317-5329, database is CAplus and MEDLINE.
Geldanamycin interferes with the action of heat shock protein 90 (Hsp90) by binding to the N-terminal ATP binding site and inhibiting an essential ATPase activity. In a program directed toward finding potent, water soluble inhibitors of Hsp90, we prepared a library of over sixty 17-alkylamino-17-demethoxygeldanamycin analogs, and compared their affinity for Hsp90, ability to inhibit growth of SKBr3 mammalian cells, and in selected cases, water solubility Over 20 analogs showed cell growth inhibition potencies similar to that of 17-allylamino-17-demethoxygeldanamycin (17-AAG), the front-runner geldanamycin analog that is currently in multiple clin. trials. Many of these analogs showed water solubility properties that were desirable for formulation. One of the most potent and water-soluble analogs in the series was 17-(2-dimethylaminoethyl)amino-17-demethoxygeldanamycin (17-DMAG), which was independently prepared by the NCI and will soon enter clin. trials. Importantly, the binding affinity of these analogs to the mol. target Hsp90 does not correlate well with their cytotoxicity in SKBr3 cells.
Bioorganic & Medicinal Chemistry published new progress about 795299-77-3. 795299-77-3 belongs to quinuclidine, auxiliary class Azetidine,Amine, name is 2-(Azetidin-1-yl)ethanamine, and the molecular formula is C19H21N3O3S, Safety of 2-(Azetidin-1-yl)ethanamine.
Referemce:
https://en.wikipedia.org/wiki/Quinuclidine,
Quinuclidine | C7H13N | ChemSpider