The post DAUNORUBICIN Synthesis, SAR, MCQ,Structure,Chemical Properties and Therapeutic Uses appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.
]]>(8S,10S)-8-Acetyl-10-[(2S,4S,5S,6S)-4-amino-5-hydroxy-6-methyl-oxan-2-yl]oxy-6,8,11-trihydroxy-1-methoxy-9,10-dihydro-7H-tetracene-5,12-dione.
Duanorubicin falls under the category of Anthracyclic antibiotic cytotoxic drug. [1]
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 527.5 g/mol |
2 | Appearance | Thin red needle form |
3 | Melting point | 208.5°C |
4 | Solubility | Soluble in methanol, chloroform and benzene |
5 | Octanol water partition coefficient | 1.83 |
6 | Presence of ring | dihydroxyanthraquinone ring |
i. Duanorubicin forms 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]
Danorubicin can be obtained from cultures of Streptomyces caeruleorubidus and Streptomyces peucetius.
TOTAL SYNTHESIS:
i. N-trifloroacetylduanosamine was obtained from duanosamine hydrochloride by ethyl acetate.
ii. The 1,4-bis(o-p—nitro-benzoate was obtained from ether acetone and suspended in CH2Cl2 at freezing temperature.
iii. It was saturated with Anhydrous HBr to give clear solution.
iv. P-nitrobenzoic acid was precipitated from the above clear solution.
v. Filteration and evaporation afforded the residual 1-bromo sugar.
vi. When the product was identified from silica gel in ethyl acetate-benzene-methanol, the impurities were separated through column chromatography.
vii. Recrystallization with 95% ethanol gives productwith 50% yield. [4]
Doxorubicin is used for the treatment of :
Q.1 Match the following with correct Trade names of the drugs-
i. Daunorubicin | A. Mustine |
ii. Mechlorethamine | B. Cirubidine |
iii. Ifosfamide | C. Dacarin |
iv. Dacarbazine | D. Holoxan |
a) i-D, ii-A, iii-B, iv-C
b) i-B, ii-A, iii-D, iv-C
c) i-C, ii-A, iii-D, iv-B
d) i-D, ii-B, iii-A, iv-C
Q.2 How many statements below are true with respect to the SAR of the drug Daunorubicin?
a) 1
b) 2
c) 3
d) 4
Q.3 The drug Daunorubicin is found in which form?
a) Thin reddish needles form
b) Yellow prism form
c) Brown poder form
d) None of the above
Q.4 The correct statement/s with respect to the method of synthesis of the drug Daunorubicin is/are?
a) Daunorubicin is obtained from cultures of Streptomyces peucetius
b) Daunorubicin is obtained from cultures of Streptomyces caeruleorubidus
c) Both a) and b)
d) None of the above
Q.5 Which amongst the following is not a therapeutic use of drug Daunorubicin?
a) AML
b) Hair loss
c) ALL
d) APL
Q.6 The correct classification of the drug Daunorubicin can be?
a) Triazine
b) Antibiotics
c) Anti folate agent
d) Pyrimidine antagonist
Q.7 How many number of rings are found in the chemical structure of the drug Daubnorubicin?
a) 5
b) 4
c) 3
d) 2
1-b
2-c
3-a
4-d
5-b
6-b
7-a
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