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Updated: Jan 26, 2026

Synthesis and Characterization of an Aspirin-fumarate Prodrug that Inhibits NFκB Activity and Breast Cancer Stem Cells

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Published on: January 18, 2017

PPh2Me促進[4+3]環化反応による抗乳がん剤としてのキナゾリン縮合ベンゾチアジアゼピン合成

Peng-Fei Sun¹, Yu-Jiao Wang¹, Ying-Hao Liao¹

¹School of Chemistry and Materials Science, Jiangsu Normal University, Xuzhou, China.

Chemistry (Weinheim an der Bergstrasse, Germany)

|January 25, 2026

Abstract:

A PPh₂Me-promoted [4 + 3] annulation between benzo[c][1,2]dithiol-3-ones and quinazoline-derived azomethine imines for the facile synthesis of a novel quinazoline-fused benzothiadiazepine library is described. This transformation is characterized by its mild conditions and excellent functional group tolerance, affording 25 novel tetracyclic compounds in excellent yields (most >85%). The biological evaluation of the obtained tetracyclic products established the scaffold's promising preliminary anti-TNBC profile. The lead compound, 3ma, further demonstrated potent anti-migratory effects in wound healing and transwell assay, suggesting anti-metastatic potential. Preliminary mechanistic insights from molecular docking studies indicated binding affinity to the EGFR kinase active site, which provides a testable hypothesis for the mechanism of action.

キーワード:

抗TNBC活性アゾメチンイミンベンゾ[c][1,2]ジチオール-3-オン分子ドッキングホスフィン

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Cercosporin-Photocatalyzed [4+1]- and [4+2]-Annulations of Azoalkenes Under Mild Conditions

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