Drug intelligence / Profile preview

bispidinone analog 9

Development stage
Preclinical
Lead developer
Inje University
Modality
Small Molecules
Administration
In Vitro
01

Overview

bispidinone analog 9 is a synthetic small molecule derived from the bispidinone scaffold (3,7-diazabicyclo[3.3.1]nonan-9-one) and distinguished by four methoxy-substituted aryl groups at positions 2, 4, 6, and 8. It was developed to explore anticancer activity and demonstrated potent cytotoxicity in HeLa cervical carcinoma cells with an IC50 of approximately 13 µM. The drug induces cell cycle arrest at sub-G1 and G1 phases, inhibits DNA replication, and triggers apoptosis via mitochondria-mediated and caspase-mediated pathways, including activation of Bax, suppression of Bcl-2, activation of caspase-3 and caspase-9, and upregulation of p53. There is also evidence suggesting effects on the extrinsic Fas-mediated apoptotic pathway.

Other names
2,4,6,8-tetrakis(2-methoxyphenyl)-3,7-diazabicyclo[3.3.1]nonan-9-one
02

Targets

BCL-2 (BCL-2 family)

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