Pyrrolo[2,1-f][1,2,4]triazine: a promising fused heterocycle to target kinases in cancer therapy

被引:10
作者
Singh, Sarbjit [1 ]
Utreja, Divya [2 ]
Kumar, Vimal [3 ]
机构
[1] Univ Nebraska Med Ctr, Eppley Inst Res Canc & Allied Dis, Omaha, NE 68198 USA
[2] Punjab Agr Univ, Dept Chem, Ludhiana 141004, Punjab, India
[3] Dr BR Ambedkar Natl Inst Technol NIT, Dept Chem, Jalandhar 144011, Punjab, India
关键词
Pyrrolo[2,1-f][1,2,4]triazine; Kinase inhibition; Fused heterocycles; Cancer; Targeted therapy; PYRROLOTRIAZINE DUAL INHIBITORS; HEDGEHOG SIGNALING PATHWAY; CELL LUNG-CANCER; HIGHLY POTENT; ANTIPROLIFERATIVE ACTIVITY; HORMONE-THERAPY; JAK INHIBITORS; IN-VITRO; DISCOVERY; EGFR;
D O I
10.1007/s00044-021-02819-1
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Cancer is the second leading cause of death worldwide responsible for about 10 million deaths per year. To date several approaches have been developed to treat this deadly disease including surgery, chemotherapy, radiation therapy, hormonal therapy, targeted therapy, and synthetic lethality. The targeted therapy refers to targeting only specific proteins or enzymes that are dysregulated in cancer rather than killing all rapidly dividing cells, has gained much attention in the recent past. Kinase inhibition is one of the most successful approaches in targeted therapy. As of 30 March 2021, FDA has approved 65 small molecule protein kinase inhibitors and most of them are for cancer therapy. Interestingly, several kinase inhibitors contain one or more fused heterocycles as part of their structures. Pyrrolo[2,1-f][1,2,4]triazine is one the most interesting fused heterocycle that is an integral part of several kinase inhibitors and nucleoside drugs viz. avapritinib and remdesivir. This review articles focus on the recent advances made in the development of kinase inhibitors containing pyrrolo[2,1-f][1,2,4]triazine scaffold.
引用
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页码:1 / 25
页数:25
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