Drug intelligence / Profile preview

NAHO27

Development stage
Preclinical
Lead developer
University of Cologne
Modality
Small Molecules
01

Overview

NAHO27 is an organometallic diarylethyne cobalt carbonyl complex designed as a cis-locked structural analogue of the natural antineoplastic agent combretastatin A-4. It selectively induces apoptosis in various cancer cell lines, including lymphoma, leukemia, breast cancer, and melanoma, while sparing normal leukocytes. The drug exerts its effects primarily through the intrinsic (mitochondrial) apoptotic pathway, characterized by the loss of mitochondrial membrane potential, processing of caspases 3 and 9, and modulation of Bcl-2 family proteins, specifically upregulating the pro-apoptotic protein Harakiri (HRK). Notably, NAHO27 demonstrates the ability to overcome multidrug resistance (MDR) mediated by p-glycoprotein and exhibits significant synergistic activity when combined with vincristine.

Other names
Hexacarbonyl[1,3-dimethoxy-5-((4′-methoxyphenyl)ethynyl)benzene]dicobaltdicobalt hexacarbonyl complex of 1,3-dimethoxy-5-((4-methoxyphenyl)ethynyl)benzene
02

Targets

BCL-2 (BCL-2 family)CASP3 (Caspase-3)CASP9 (Caspase-9)SMAC

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