Abstract
The application of privileged structures in drug design is an effective strategy, which
usually leads to innovative hits/leads and successful structural optimization. Pyrrolo[2, 3-
d]pyrimidine are such a scaffold which are frequently used in many clinical drugs. The biocompounds
bearing pyrrolo[2, 3-d]pyrimidine skeleton show different pharmacological effects such as
anti-neurodegenerative, anti-inflammatory, antibacterial, and antitumor activities. In this article, we
reviewed the representative structures and biological characteristics of reported synthetic pyrrolo[2,
3-d]pyrimidine compounds from 2017 to 2021. The linked diseases and targets were also mentioned
briefly. This work might provide a reference for the subsequent drug discovery based on pyrrolo[2,
3-d]pyrimidine scaffold.
Graphical Abstract
[21]
Watterson, S.H.; De Lucca, G.V.; Shi, Q.; Langevine, C.M.; Liu, Q.; Batt, D.G.; Beaudoin Bertrand, M.; Gong, H.; Dai, J.; Yip, S.; Li, P.; Sun, D.; Wu, D.R.; Wang, C.; Zhang, Y.; Traeger, S.C.; Pattoli, M.A.; Skala, S.; Cheng, L.; Obermeier, M.T.; Vickery, R.; Discenza, L.N.; D’Arienzo, C.J.; Zhang, Y.; Heimrich, E.; Gillooly, K.M.; Taylor, T.L.; Pulicicchio, C.; McIntyre, K.W.; Galella, M.A.; Tebben, A.J.; Muckelbauer, J.K.; Chang, C.; Rampulla, R.; Mathur, A.; Salter-Cid, L.; Barrish, J.C.; Carter, P.H.; Fura, A.; Burke, J.R.; Tino, J.A. Discovery of 6-Fluoro-5-(
R )-(3-(
S )-(8-fluoro-1-methyl-2,4-dioxo-1,2-dihydroquinazolin-3(4 H )-yl)-2-methylphenyl)-2-(
S )-(2-hydroxypropan-2-yl)-2,3,4,9-tetrahydro-1 H -carbazole-8-carboxamide (BMS-986142): A Reversible Inhibitor of Bruton’s Tyrosine Kinase (BTK) Conformationally Constrained by Two Locked Atropisomers.
J. Med. Chem., 2016,
59(19), 9173-9200.
[
http://dx.doi.org/10.1021/acs.jmedchem.6b01088] [PMID:
27583770]