Design and synthesis of 7-azaindole derivatives as potent CDK8 inhibitors for the treatment of acute myeloid leukemia.

It is of great significance to design and synthesize novel structural inhibitors with good antitumor activity. In this study, based on rational design, a total of 42 7-azaindole derivatives as novel CDK8 inhibitors were designed and synthesized. All compounds were screened with antitumor activity and compound 6 (1-(3-((1-pyrrolo[2,3-]pyridin-5-yl)oxy)phenyl)-3-(-tolyl)urea) exhibited the best activity, especially in acute myeloid leukemia (GI MV4-11 = 1.