Drug intelligence / Profile preview

thiosemicarbazide derivative of captopril

Development stage
Preclinical
Lead developer
Basrah University
Modality
Small Molecules
Administration
In Vitro, Unknown
01

Overview

A thiosemicarbazide derivative of captopril is a novel small molecule in which a thiosemicarbazide moiety is chemically integrated into the structure of captopril, an angiotensin-converting enzyme inhibitor. Several derivatives have been synthesized and investigated, and one in particular (often denoted as derivative 8) shows notable antiproliferative activity against breast cancer cell lines, particularly MCF-7 (estrogen receptor positive) and AMJ13 (estrogen/progesterone receptor negative). This compound exhibits a mixed mode of cell death, inducing both apoptotic (via caspase-3 and caspase-9 involvement, with ROS generation) and non-apoptotic pathways depending on cell context. Additionally, it has demonstrated antiangiogenic effects and significant antiplatelet and ACE inhibitory activity in vitro. The inclusion of thiosemicarbazide enhances the spectrum of biological activities, seeking to improve on the cardiovascular properties of the original captopril scaffold while introducing notable anticancer and antiplatelet potential[2][4][5][7].

Other names
captopril thiosemicarbazide derivativederivative 8derivative8derivative-8compound 8compound8compound-8
02

Targets

ACE (Angiotensin Converting Enzyme)GPIIb/IIIa (Integrin alpha-IIb/beta-3)PGHS-1 (Prostaglandin G/H Synthase 1)P2Y12 (Purinergic P2Y12 receptor)

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