Angiogenesis and anti-leukaemia activity of novel indole derivatives as potent colchicine binding site inhibitors

Yongfang Yao, Tao Huang, Yuyang Wang, Longfei Wang, Siqi Feng, Weyland Cheng, Longhua Yang & Yongtao Duan
The screened compound DYT-1 from our in-house library was taken as a lead (inhibiting tubulin polymerisation: IC50=25.6 µM, anti-angiogenesis in Zebrafish: IC50=38.4 µM, anti-proliferation against K562 and Jurkat: IC50=6.2 and 7.9 µM, respectively). Further investigation of medicinal chemistry conditions yielded compound 29e (inhibiting tubulin polymerisation: IC50=4.8 µM and anti-angiogenesis in Zebrafish: IC50=3.6 µM) based on tubulin and zebrafish assays, which displayed noteworthily nanomolar potency against a variety of leukaemia cell lines (IC50= 0.09–1.22 µM), especially...
1 citation reported since publication in 2022.
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