Category: indole-building-blockIn 2010, Shen, Zhongqi;Siva Ramamoorthy, P.;Hatzenbuhler, Nicole T.;Evrard, Deborah A.;Childers, Wayne;Harrison, Boyd L.;Chlenov, Michael;Hornby, Geoffrey;Smith, Deborah L.;Sullivan, Kelly M.;Schechter, Lee E.;Andree, Terrance H. published 《Synthesis and structure-activity relationship of novel lactam-fused chroman derivatives having dual affinity at the 5-HT1A receptor and the serotonin transporter》. 《Bioorganic & Medicinal Chemistry Letters》published the findings. The article contains the following contents:
The structure-activity relationship (SAR) for three series of lactam-fused chroman derivatives possessing 3-amino substituents was evaluated. Many compounds exhibited affinities for both the 5-HT1A receptor and the 5-HT transporter. I [R = F, CN] demonstrated 5-HT1A antagonist activities in the in vitro cAMP turnover model.6-Methoxyisoindolin-1-one (cas: 132680-54-7) were involved in the experimental procedure.
The crystal structure of 6-Methoxyisoindolin-1-one(cas:132680-54-7 Category: indole-building-block) has been determined using x-ray crystallography and cell studies. It was found that 6-Methoxyisoindolin-1-one inhibits the interactions of chk1 with substructures of DNA, such as the major groove and minor groove.
Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles