Drug intelligence / Profile preview

2',5'-dimethoxychalcone compound 2

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

2',5'-dimethoxychalcone compound 2 is a synthetic small molecule chalcone derivative investigated for its dual antiplatelet and antineoplastic activities. It serves as a potent inhibitor of Cyclooxygenase-1 (COX-1), binding directly to the enzyme's active site to suppress the formation of thromboxane B2 and inhibit collagen-induced platelet aggregation. In addition to its antiplatelet effects, the compound has demonstrated antiproliferative activity against human bladder cancer cell lines (such as NTUB1). Its anticancer mechanism involves the induction of G1 phase cell cycle arrest through a COX-1 independent pathway, characterized by the increased expression of the cyclin-dependent kinase inhibitors p21 and p27 and a reduction in reactive oxygen species levels.

Other names
2',5'-dimethoxychalcone
02

Targets

PGHS-1 (Prostaglandin G/H Synthase 1)CDKN1B (Transmembrane emp24 domain-containing protein 7)CDKN1A (Cyclin-dependent kinase inhibitor 1A)

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