Zhou, Nan published the artcileDiscovery of a tetrahydroisoquinoline-based HDAC inhibitor with improved plasma stability, Application In Synthesis of 142335-42-0, the publication is Bioorganic & Medicinal Chemistry (2017), 25(17), 4614-4619, database is CAplus and MEDLINE.
Histone deacetylase inhibitors with desirable pharmacokinetic profiles which can be delivered to solid tumor tissues in large amount might be promising to treat solid tumor effectively. Herein, structural modification of a previously reported tetrahydroisoquinoline-based HDAC inhibitor 2-[(2S,3S)-2-[(3,3-dimethyl-1-oxobutyl)amino]-3-methyl-1-oxopentyl]-1,2,3,4-tetrahydro-7-[2-(hydroxyamino)-2-oxoethoxy]-N-(4-methoxyphenyl)-, (3S)-3-Isoquinolinecarboxamide [1314556-93-8] (I) was carried out to improve its plasma stability for more feasible drug delivery. Among three newly synthesized analogs, the in vitro rat plasma stability of compound (II) (t1/2 = 630 min) was over 5-fold improved than its parent I (t1/2 = I03 min). In vitro activity evaluation showed that compound II and I exhibited similar HDACs inhibitory activity, which was validated by western blot anal. and antiproliferative assay. Moreover, compared with I, compound II exhibited comparable, if not higher, in vivo antitumor activity in a human breast carcinoma (MDA-MB-231) xenograft model.
Bioorganic & Medicinal Chemistry published new progress about 142335-42-0. 142335-42-0 belongs to tetrahydroisoquinoline, auxiliary class Tetrahydroisoquinoline,Chiral,Carboxylic acid,Amide,Alcohol, name is (S)-2-(tert-Butoxycarbonyl)-7-hydroxy-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid, and the molecular formula is C9H6FNO, Application In Synthesis of 142335-42-0.
Referemce:
https://en.wikipedia.org/wiki/Tetrahydroisoquinoline,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem