Drug intelligence / Profile preview

4-ethyl-N-(3,4-dihydroisoquinolin-2(1H)-yl)benzamide

Development stage
Preclinical
Lead developer
Florida Agricultural and Mechanical University
Modality
Small Molecules
01

Overview

4-ethyl-N-(3,4-dihydroisoquinolin-2(1H)-yl)benzamide (also known as GM-3-121) is a synthetic tetrahydroisoquinoline (THIQ) derivative developed by researchers at Florida A&M University. It was designed as an anti-angiogenic and anti-cancer agent. GM-3-121 has demonstrated potent anti-proliferative activity against breast cancer cell lines (including MCF-7 and triple-negative MDA-MB-231) and endometrial adenocarcinoma (Ishikawa) cells. It acts as a cytostatic agent that halts cell cycle progression at the G2/M phase by holding the microtubule network static and preventing mitosis, without functioning as a spindle poison. Additionally, GM-3-121 exhibits anti-angiogenic properties, inhibiting the formation of new blood vessels by targeting the VEGF pathway, and has shown activity as a KRas inhibitor in colorectal cancer models.

Other names
4-ethyl-N-(3,4-dihydroisoquinolin-2(1H)-yl) benzamide
02

Targets

TUBB (Tubulin (alpha and beta subunits))KRAS (Kirsten rat sarcoma viral oncogene homolog)VEGFR (VEGFR family)

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