Design, synthesis and biological evaluation of N-arylsulfonyl carbazoles as novel anticancer agents

N-芳基磺酰基咔唑类化合物作为新型抗癌剂的设计、合成及生物学评价

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Abstract

In this work, a set of structurally diverse synthetic carbazoles was screened for their anticancer activities. According to structure-activity relationship studies, carbazoles with an N-substituted sulfonyl group exhibited better anticancer activity. Moreover, compound 8h was discovered to show the most potent anticancer effects on Capan-2 cells by inducing apoptosis and cell cycle arrest in G2/M phase. Finally, the in vivo study demonstrated that 8h prevented the tumor growth in PANC-1 and Capan-2 xenograft models without apparent toxicity.

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