Compound ID | 2087

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Holomycin

Class: RNA polymerase inhibitor (dithiolopyrrolone)

Agent Type: Natural product; Small molecule; Direct acting;
Spectrum of activity: Gram-positive & Gram-negative
Mechanism of action: RNA synthesis inhibitor. DNA-dependent RNA polymerase inhibitor; prodrug that needs to be activated in cells
Description: Natural product produced by several species of Streptomyces, Saccharothrix and Gram-negative bacteria; total synthesis and several analogues; related to Pseudomonic acid A (mupirocin). Activity as angiogenesis inhibitor and antineoplastic agent
Year first mentioned: 1959
Development status: Experimental
Reason dropped: Toxic
Chemical structure(s):
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Molecular weight: 214.27
Iso. SMILES: CC(=O)NC1=C2C(=CSS2)NC1=O
InChI Key: HBUNPJGMNVQSBX-UHFFFAOYSA-N
Can. SMILES: CC(=O)NC1=C2C(=CSS2)NC1=O
InChI: InChI=1S/C7H6N2O2S2/c1-3(10)8-5-6-4(2-12-13-6)9-7(5)11/h2H,1H3,(H,8,10)(H,9,11)
External links:
PubChem link: https://pubchem.ncbi.nlm.nih.gov/compound/10262683
Citations:
  • https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3826145/
  • https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4132845/
  • https://pubmed.ncbi.nlm.nih.gov/24323287/

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