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

doxorubicin 2 

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

etoposide 2

Synonyms: VP-16

Source: Semi-synthetic derivative of podophyllotoxin fromPodophyllum 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

teneposide

Synonyms: VP-26

Source: Semi-synthetic derivative of podophyllotoxin fromPodophyllum 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

mamsa 1

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

actino n

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

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

 

topotecan 2

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

ellipticine 2

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

icrf193 2

Source:

Formula: C12N4O4H18

M. Wt.: 282.3 g/mol

Solubility: Soluble in DMSO (4 mg/ml)