Structure-activity relationship study of novel evodiamine amino acid conjugates with potent anti-colorectal cancer efficacy.

Evodiamine has been a promising lead structure with broad-spectrum antitumor activity. Druggability optimization is the most challenging part of evodiamine-based lead-to-candidate campaign. Amino acids as building blocks for conjugates are widely incorporated into approved drug and drug candidates, demonstrating highly attractive druggability.

Exploring the Therapeutic Effects of Multifunctional -Salicylic Acid Tryptamine Derivative against Parkinson's Disease.

Parkinson's disease (PD) is the second most common neurodegenerative disease worldwide. Neuroinflammation and oxidative stress play an important role in the whole course of PD, which have been the focus of PD drug development. In our previous research, a series of -salicylic acid tryptamine derivatives were synthesized, and the biological evaluation showed that the compound 02003 has good anti-neuroinflammatory activity and displayed great therapeutic potency for neurodegenerative disease models.

Development of -aminobenzamide salt derivatives for improving water solubility and anti-undifferentiated gastric cancer.

Gastric cancer is one of the cancers with wide incidence, difficult treatment and high mortality in the world, especially in Asia and Africa. In our previous work, a novel -aminobenzamide analogue was identified as an early preclinical candidate for treatment of undifferentiated gastric cancer (IC of 0.26 μM for HGC-27).

Natural product evodiamine-inspired medicinal chemistry: Anticancer activity, structural optimization and structure-activity relationship.

It is a well-known phenomenon that natural products can serve as powerful drug leads to generate new molecular entities with novel therapeutic utility. Evodiamine (Evo), a major alkaloid component in traditional Chinese medicine Evodiae Fructus, is considered a desirable lead scaffold as its multifunctional pharmacological properties. Although natural Evo has suboptimal biological activity, poor pharmacokinetics, low water solubility, and chemical instability, medicinal chemists have succeeded in producing synthetic analogs that overshadow the deficiency of Evo in terms of further clinical application.

-2-(Phenylamino) Benzamide Derivatives as Dual Inhibitors of COX-2 and Topo I Deter Gastrointestinal Cancers via Targeting Inflammation and Tumor Progression.

Given the close association between inflammation and cancer, combining anti-inflammation therapy is prominent to improve the anticancer effect. Based on , a series of agents targeting COX-2 and Topo I were designed by combining fenamates and phenols. The optimal compound displayed an enhanced inhibitory effect on COX-2 compared to tolfenamic acid and and showed better inhibition of Topo I than .

Design, Synthesis, and Biological Evaluation of Novel Evodiamine Derivatives as Potential Antihepatocellular Carcinoma Agents.

Evodiamine has many biological activities. Herein, we synthesize 23 disubstituted derivatives of N14-phenyl or the E-ring of evodiamine and conduct systematic structure-activity relationship studies. antiproliferative activity indicated that compounds and dramatically inhibited the proliferation of Huh7 (IC = 0.