Anti-cancer Agents

ANTHRACYCLINES

Target: Eukaryotic topoisomerase II inhibitors. Thought to act as a poison of the enzyme, stabilising the covalent complex between DNA and enzyme leading to an accumulation of cytotoxic DNA breaks in cells.

  • Doxorubicin

 

      

Synonyms: 14-Hydroxydaunorubicin

Source: Synthetic

Formula: C27H29O11N

M.Wt.: 543.5 g/mol

Solubility: Soluble in water (10 mg/ml), DMSO and ethanol

    

     

    

    

    

EPIPODOPHYLLOTOXINS

Target: Eukaryotic topoisomerase II inhibitors. Thought to act as a poison of the enzyme, stabilising the covalent complex bewteen DNA and enzyme leading to an accumulation of cytotoxic DNA breaks in cells.

  • Etoposide

 

Synonyms: VP-16

Source: Semi-synthetic derivative of podophyllotoxin from Podophyllum peltatum.

Formula: C29H32O13

M.Wt.: 588.6 g/mol

Solubility: Poorly soluble in water (0.2 mg/ml) and ethanol (1 mg/ml), soluble in DMSO (> 100 mg/ml).

     

     

     

     

     

     

     

     

     

     

    

   

  •  Teniposide

    

    

      

Synonyms: VP-26

Source: Semi-synthetic derivative of podophyllotoxin from Podophyllum peltatum.

Formula: C32H32O13S

M. Wt.: 656.7 g/mol

Solubility: Poorly soluble in water (< 1 mg/ml) and ethanol (1 mg/ml), soluble in DMSO (> 100 mg/ml).      

     

     

     

     

     

     

     

     

     

     

     

     

 ACRIDINES

Target: Eukaryotic topoisomerase II inhibitors. Thought to act as poisons of the enzyme, stabilising the covalent complex bewteen DNA and enzyme leading to an accumulation of cytotoxic DNA breaks in cells.

  • mAMSA

 

       

Synonyms: Amsacrine

Formula: C21H19N3O3S

M. Wt.: 393.5 g/mol

Solubility: Poorly soluble in water (< 1 mg/ml) and ethanol (2 mg/ml), soluble in DMSO (> 100 mg/ml).

    

     

    

     

     

     

ACTINOMYCINS

  • Actinomycin D

       

Synonyms: Dactinomycin

Source:  Streptomyces parvelus

Formula: C62H86N12O16

M. Wt.: 1255.4 g/mol

Solubility: Slightly soluble in water (0.5 mg/ml), soluble in DMSO (> 1 mg/ml).

    

    

   

    

  

CAMPTOTHECIN ANALOGS

Target: Eukaryotic topoisomerase I inhibitors. Act by binding to both enzyme and DNA and so stabilise the complex between them.

  • Camptothecin

 

         

Source:Camptotheca acuminata

Formula: C20H16N2O4

M. Wt.: 384.4 g/mol

Solubility: Poorly soluble in water (< 1 mg/ml) and ethanol, soluble in DMSO (5 mg/ml).

    

    

    

  

    

  •  Topotecan

  

    

    

Source: Semi-synthetic water soluble derivative of camptothecin

Formula: C23H23N3O5

M.Wt.: 421.5 g/mol

Solubility: Soluble in water (1 mg/ml)

   

  

  

  

   

ELLIPTICINE AND ANALOGUES

Target: Eukaryotic topoisomerase II inhibitors. Thought to act as a poisons of the enzyme, intercalating into the DNA and increasing the cleavage reaction leading to an accumulation of cytotoxic DNA breaks in cells.

  • Ellipticine

 

    

Source:  Ochrosia elliptica

Formula: C17H14N2

M. Wt.: 246.3 g/mol

Solubility: Soluble in DMSO and ethanol

  

  

  

  

  

  

BISDIOXOPIPERAZINES

Target: Eukaryotic topoisomerase II inhibitors. Catalytic inhibitors which interfere with ATPase and DNA strand-passage reactions leading to stabilisation of the closed clamp form of the enzyme.

  • ICRF-193

Source:

Formula: C12N4O4H18

M. Wt.: 282.3 g/mol

Solubility: Soluble in DMSO (4 mg/ml)