Drug intelligence / Profile preview

compound 14b

Development stage
Preclinical
Lead developer
Mansoura University
Modality
Small Molecules
Administration
Oral
01

Overview

Compound 14b is a synthetic, small-molecule nitric oxide (NO)-releasing analog of estra-1,3,5,16-tetraene. It was developed as a dual-action therapeutic agent designed to overcome multidrug resistance (MDR) in hepatocellular carcinoma (HCC). Chemically, it is the S-isomer of a series of nitric oxide-releasing estra-1,3,5,16-tetraene analogs (NO-∆-16-CIEAs). Its mechanism of action involves the inhibition of the epidermal growth factor receptor (EGFR) and the multidrug resistance-associated protein 2 (MRP2), alongside the release of nitric oxide, which collectively sensitize cancer cells to chemotherapy. In preclinical models, compound 14b demonstrated significant anti-proliferative activity against both standard (HepG2) and resistant (HepG2-R) liver cancer cell lines, showing higher potency than the reference EGFR inhibitor erlotinib.

Other names
(S)-isomer of nitric oxide-releasing estra-1,3,5,16-tetraene analogNO-∆-16-CIEA 14b
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)MRP2 (Canalicular multispecific organic anion transporter 1)

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