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  • Title: Design, synthesis, and biological evaluation of diaryl heterocyclic derivatives targeting tubulin polymerization with potent anticancer activities.
    Author: Li G, Wu JQ, Cai X, Guan W, Zeng Z, Ou Y, Wu X, Li J, Fang X, Liu J, Zhang Y, Wang H, Yin C, Yao H.
    Journal: Eur J Med Chem; 2023 Apr 05; 252():115284. PubMed ID: 36940610.
    Abstract:
    A series of diaryl heterocyclic analogues were designed and synthesized as tubulin polymerization inhibitors. Among them, compound 6y showed the highest antiproliferative activity against HCT-116 colon cancer cell line with an IC50 values of 2.65 μM. Compound 6y also effectively inhibited tubulin polymerization in vitro (IC50 of 10.9 μM), and induced HCT-116 cell cycle arrest in G2/M phase. In addition, compound 6y exhibited high metabolic stability on human liver microsomes (T1/2 = 106.2 min). Finally, 6y was also effective in suppressing tumor growth in a HCT-116 mouse colon model without apparent toxicity. Collectively, these results suggest that 6y represents a new class of tubulin inhibitors deserving further investigation.
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