FTO has been recognized as a promising therapeutic target for acute myeloid leukemia (AML). However, the development of FTO inhibitors with anti-leukemia effects was still limited. Here, based on reasonable design and SAR, a total of 67 compounds were synthesized, among which compound E6 exhibited the strongest activ...
Yu-Meng Wang, Ya-Ting Lu, Hao-Dong Liu et al.· Journal of Medicinal Chemist...· 0 citations
H-10 elicited dose-dependent seizure suppression and alleviated multi-organ pathological damage in both acute and chronic epileptic mouse models and is an orally bioavailable, efficacious GABAAR-targeted PAM with broad-spectrum antiseizure activity, deserving further optimization for anticonvulsant drug discovery.
Di Hu, Ying Wang, Jin-Ling Yu et al.· European journal of medicina...· 0 citations
LW-1 represents a promising CDK8 inhibitor with improved drug-like properties and potent anti-psoriatic efficacy, providing a potential therapeutic candidate for the treatment of psoriasis and other inflammatory diseases.
Cen-Cen Lei, Dawei Jin, A-Jun Liu et al.· Bioorganic chemistry (Print)· 0 citations
Camptothecin (CPT) and its derivatives are clinically validated topoisomerase I (Topo I) inhibitors with broad-spectrum antitumor activity and modification at the 10-position of the CPT scaffold represents a promising strategy to enhance binding affinity.
Yixuan Zhang, Hong Wang, Feilong Zhou et al.· European journal of medicina...· 0 citations
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