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]]>(7S,9S)-7-[(2R,4S,5S,6S)-4-Amino-5-hydroxy-6-methyloxan-2-yl]oxy-6,9,11-trihydroxy-9-(2-hydroxyacetyl)-4-methoxy-8,10-dihydro-7H-tetracene-5,12-dione.
Doxorubicin falls under the category of Anthracyclic antibiotic cytotoxic drug. [1]
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 543.5 g/mol |
2 | Appearance | Red crystalline solid |
3 | Melting point | Range between 229-231°C |
4 | Solubility | Soluble in water |
5 | Octanol water partition coefficient | 1.27 |
6 | Presence of ring | Anthraquinone ring system. |
i. Doxorubicin firms complexes with DNA by intercalation between base pairs.
ii. The drug then stabilizes DNA-topoisomerase II and thus topoisomerase activity is inhibited.
iii. Relegation of the DNA is prevented.
iv. Cell death. [2]
i. In the first step, adriamycinone converts into dioxolone derivative.
ii. It is then condensed with N-O-ditriflouroacetyl-alpha-daunosaminyl chloride.
iii. The formed compound is then treated with methanol to remove the O-triflouroacetyl group.
iv. First alkaline and then an acid treatment is given to the compound to give doxorubicin.
Doxorubicin is used for the treatment of :
Q.1 What can be the correct Trade name for Doxorubicin?
a) Irinotel
b) Dacmozen
c) Oncotron
d) Adriamycin
Q.2 Which amongst the following statements is/are incorrect related to the SAR of Doxorubicin?
I. Substitution at 2nd position will increase the biological activity of drug.
II. Substitution at 1st and 7th position will have negative impact on the biological activity of the drug.
III. Substitution at 1st and 7th position will have negative impact on the biological activity of the drug.
a) I, II & III
b) I & II
c) I
d) II & III
Q.3 The correct order for the mechanism of action of Doxorubicin can be?
I. Stabilization of DNA-Topoisomerase II complex
II. Intercalation between DNA base pairs
III. Relegation of DNA is prevented
a) I – II – III
b) II – I – III
c) III – I – II
d) III – II – I
Q.4 The drug Doxorubicin is mainly used for?
a) Treatment of cancers
b) As an antiviral drug
c) Antiarrytthmic drug
d) Both a) and c)
Q.5 Match the drugs with the correct classification.
i. Doxorubicin | A. Aromatase inhibitors |
ii. Busulfan | B. Vinca alkaloids |
iii. Vinblastin | C. Alkyl sulfonate |
iv. Exemestane | D. Antibiotics |
a) i-A, ii-B, iii-C, iv-D
b) i-D, ii-C, iii-B, iv-A
c) i-C, ii-D, iii-B, iv-A
d) i-D, ii-C, iii-A, iv-B
Q.6 How many statements below are true with respect to the side effects of the drug Doxorubicin?
a) 2
b) 3
c) 4
d) 1
Q.7 The type of ring system found in Doxorubicin is?
a) No ring system present
b) Pyrimidine ring system
c) Purine ring system
d) Anthraquinone ring system
1-d
2-c
3-b
4-a
5-b
6-c
7-d
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