663595-69-5Relevant academic research and scientific papers
Design, structure-activity relationship study and biological evaluation of the thieno[3,2-c]isoquinoline scaffold as a potential anti-cancer agent
Liu, Jiang Tian,Jaunky, Dilan B.,Larocque, Kevin,Chen, Fei,Mckibbon, Keegan,Sirouspour, Mehdi,Taylor, Sarah,Shafeii, Alexandre,Campbell, Donald,Braga, Helena,Piekny, Alisa,Forgione, Pat
supporting information, (2021/10/04)
Several derivatives of a series that share a thienoisoquinoline scaffold have demonstrated potent activity against cancer cell lines A549, HeLa, HCT-116, and MDA-MB-231 in the submicromolar concentration range. Structure-activity relationship (SAR) studies on a range of derivatives aided in identifying key pharmacophores in the lead compound. A series of compounds have been identified as the most promising with submicromolar IC50 values against a lung cancer cell line (A549). Microscopy studies of cancer cells treated with the lead compound revealed that it causes mitotic arrest and disrupts microtubules. Further evaluation via an in vitro microtubule polymerization assay and competition studies indicate that the lead compound binds to tubulin via the colchicine site.
THIOPHENE-2-CARBOXAMIDE DERIVATIVES AS MODULATORS OF CCR9 RECEPTOR
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Page/Page column 63-64, (2009/05/29)
Provided are compounds of Formula (I) or of Formula (II) that are modulators of CCR9 receptor activity, compositions containing the compounds and methods of use of the compounds and compositions. In certain embodiments, provided are methods for treating or amelioratin diseases associated with modulation of CCR9 receptor activity.
