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CLEFMA

Development stage
Preclinical
Modality
Small Molecules
01

Overview

CLEFMA is a synthetic curcumin derivative, specifically a diphenyldihalogeno-analog of curcumin, designed to enhance the anti-tumor potency and bioavailability of the parent compound. It functions as an antineoplastic agent by inducing both the intrinsic (mitochondrial) and extrinsic (death receptor) apoptotic pathways in cancer cells. The mechanism of action involves the activation of the Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) and p38 mitogen-activated protein kinase (MAPK) signaling pathways. This activation leads to the downstream activation of caspases, including caspase-3, caspase-8, and caspase-9, and the subsequent cleavage of poly(adenosine diphosphate-ribose) polymerase (PARP). CLEFMA has demonstrated significant inhibitory effects on the viability of various cancer cell lines, including uterine cervical cancer and lung cancer, making it a candidate for further oncological research.

Other names
4-[3,5-bis(2-fluorobenzylidene)-4-oxo-piperidine-1-yl]-4-oxo-2-butenoic acidEF24-fluorinated analogEF-24-fluorinated analogEF 24-fluorinated analog
02

Targets

ADRM1 (Proteasome regulatory particle subunit RPN13)

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