Design, Synthesis, and Evaluation of 3,5-Disubstituted 7-Azaindoles as Trk Inhibitors with Anticancer and Antiangiogenic Activities

Cited 53 time in webofscience Cited 0 time in scopus
  • Hit : 256
  • Download : 0
Tropomyosin-related kinase A (TrkA) is considered a promising target in the development of a therapeutic treatment of cancer and pain. In this study, we designed and synthesized a series of novel 7-azaindole-based Trk kinase inhibitors through the structure-based design strategy. By varying the functional groups at the 3 and 5 positions of a 7-azaindole scaffold, we studied the structure-activity relationships (SAR) profiles and identified a series of potent Trk inhibitors. Representative derivatives showed desirable activity in cellular proliferation and apoptosis assays. Moreover, these inhibitors exhibited noteworthy antiangiogenic activity.
Publisher
AMER CHEMICAL SOC
Issue Date
2012-06
Language
English
Article Type
Article
Keywords

NERVE GROWTH-FACTOR; KINASE INHIBITORS; BREAST-CANCER; IDENTIFICATION; METASTASIS; DISCOVERY; CELLS

Citation

JOURNAL OF MEDICINAL CHEMISTRY, v.55, no.11, pp.5337 - 5349

ISSN
0022-2623
DOI
10.1021/jm3002982
URI
http://hdl.handle.net/10203/102345
Appears in Collection
CH-Journal Papers(저널논문)
Files in This Item
There are no files associated with this item.
This item is cited by other documents in WoS
⊙ Detail Information in WoSⓡ Click to see webofscience_button
⊙ Cited 53 items in WoS Click to see citing articles in records_button

qr_code

  • mendeley

    citeulike


rss_1.0 rss_2.0 atom_1.0