Russian Journal of General Chemistry

, Volume 87, Issue 12, pp 3029–3035 | Cite as

Design, Synthesis, and Biological Evaluation of 1,4-Bis(2,3-dihydro-5-oxopyrrol-4-yl)-1,3-butadienes as Potential Chk1 Inhibitors

Letters to the Editor


A series of 1,4-bis(2,3-dihydro-5-oxopyrrol-4-yl)-1,3-butadienes were designed as inhibitors of checkpoint kinase 1 (Chk1), based on the structure‒activity relationships for known inhibitors through docking simulations. The docking results suggested that the title compounds were similar to known inhibitors in interaction with the catalytic site of Chk1. Twelve compounds were synthesized by a one-pot procedure from amines, dimethyl acetylenedicarboxylate, and glyoxal in water in the presence of catalytic amounts of γ-cyclodextrin. The inhibitory activities of the synthesized compounds were evaluated in vitro using EC9706 esophageal cancer cells. The results indicated that 1,4-bis(2,3-dihydro-5-oxopyrrol-4-yl)-1,3-butadienes significantly inhibited Chk1 (IC50 10.45 μM).


Chk1 inhibitors 1,4-bis(2,3-dihydro-5-oxopyrrol-4-yl)-1,3-butadienes synthesis biological testing 


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© Pleiades Publishing, Ltd. 2017

Authors and Affiliations

  1. 1.College of Life Science and BioengineeringBeijing University of TechnologyBeijingChina

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