Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2020 Dec 15;28(24):115830.
doi: 10.1016/j.bmc.2020.115830. Epub 2020 Oct 30.

Azaindole therapeutic agents

Damoder Reddy Motati  1 , Radhika Amaradhi  1 , Thota Ganesh  2
Affiliations

Azaindole therapeutic agents

Damoder Reddy Motati et al. Bioorg Med Chem. .

Abstract

Azaindole structural framework is an integral part of several biologically active natural and synthetic organic molecules; and several FDA approved drugs for various diseases. In the last decade, quite a number of literature reports appeared describing the pharmacology, biological activity and therapeutic applications of a variety of azaindole molecules. This prompted the organic and medicinal chemistry community to develop novel synthetic methods for various azaindoles and test them for a bioactivity against a variety of biological targets. Herein, we have summarized the biological activity of therapeutically advanced clinical candidates and several preclinical candidate drugs that contain azaindole structural moiety.

Keywords: BMS626529; Fevipiprant and HIV treatment; Guitarrins; PLX4720; Pexidartinib.

PubMed Disclaimer

Conflict of interest statement

CONFLICTS OF INTEREST

There are no conflicts to declare.

Declaration of interests

The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

Figures

Fig. 1:
Fig. 1:
Azaindoles and their chemical names and biophysical properties (calculated using ChemDraw software 16.0).
Fig. 2:
Fig. 2:
Azaindole natural products and synthetic derivatives.
Fig. 3:
Fig. 3:
FDA approved drugs and clinical candidates with the azaindole core unit.
Fig. 4:
Fig. 4:
Clinical candidates and promising molecules of azaindole derivatives.
Fig. 5:
Fig. 5:
Azaindole derivatives that displayed promising biological activity.
Fig. 6:
Fig. 6:
Bioactive azaindole derivatives.
Fig. 7:
Fig. 7:
Additional biologically interesting azaindole derivatives.
See this image and copyright information in PMC

References

    1. Walker SR, Carter EJ, Huff BC, Morris JC, Variolins and Related Alkaloids, Chem. Rev, 109 (2009) 3080–3098. - PubMed
    1. Zhao S-B, Wang S, Luminescence and Reactivity of 7-Azaindole Derivatives and Complexes, Chem. Soc. Rev, 39 (2010) 3142–3156. - PubMed
    1. Merour J-Y, Joseph B, Synthesis and Reactivity of 7-Azaindoles (1H-pyrrolo[2,3-b]pyridines), Curr. Org. Chem, 5 (2001) 471–506.
    1. Echalier A, Bettayeb K, Ferandin Y, Lozach O, Clelment M, Valette A, Liger F, Marquet B, Morris JC, Endicott JA, Joseph B, Meijer L, Meriolins (3-(Pyrimidin-4-yl)-7-azaindoles): Synthesis, Kinase Inhibitory Activity, Cellular Effects, and Structure of a CDK2/Cyclin A/Meriolin Complex, J. Med. Chem, 51 (2008) 737–751. - PubMed
    1. Ermoli A, Bargiotti A, Brasca MG, Ciavolella A, Colombo N, Fachin G, Isacchi A, Menichincheri M, Molinari A, Montagnoli A, Pillan A, Rainoldi S, Sirtori FR, Sola F, Thieffine S, Tibolla M, Valsasina B, Volpi D, Santocanale C, Vanotti E, Cell Division Cycle 7 Kinase Inhibitors: 1H-Pyrrolo[2,3-b]pyridines, Synthesis and Structure-Activity Relationships, J. Med. Chem, 52 (2009) 4380–4390. - PubMed

Publication types

MeSH terms

LinkOut - more resources