The post LOMUSTINE Synthesis, SAR, MCQ,Chemical Structure and Therapeutic Uses appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.
]]>IUPAC nomenclature
1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea
Lomustine falls under the category of alkyl Nitrosoureas alkalyting agents.
S. NO. | PHYSICAL AND CHEMICAL PROPERTIES | |
1 | Molecular weight | 233.69 g/mol |
2 | Appearance | Solid yellow powder |
3 | Melting point | 89°C |
4 | Solubility | Freely soluble in chloroform, soluble in acetone |
5 | Octanol water partition coefficient | 2.83 |
6 | Presence of ring | Cyclohexyl ring |
Carmustine is synthesized through nitrosation of 1-(2-chloroethyl)-3-cyclohexylurea in cold and acidic medium.
Q.1 What can be the correct IUPAC nomenclature of Lomustine
a) 1-(2-chloroethyl)-3-cyclohexyl-2-nitrosourea
b) 1-(2-chloroethyl)-3-cyclohexyl-1-nitrosourea
c) 1,3-Bis(2-chloroethyl)-1-nitrosourea
d) 1,3-Bis(2-chloroethyl)-2-nitrosourea
Q.2 Which amongst the following statements is/are incorrect related to the SAR of Lomustine?
I. The introduction of the substituted phenyl group will increases the oral route availability of the drug.
II. Aromatic ring introduction will decrease the stability of the drug.
III. Benzimidazole ring can provide the local and faster action of the drug.
a) I and III
b) I and II
c) II and III
d) Only II
Q.3 The correct order for the mechanism of action of Lomustine can be?
I. Apoptosis of cell
II. Alkylation of DNA
III. Hydrolysis of drug
IV. Conversion of drugs into its metabolites
a) III – IV – II – I
b) II – III – IV – I
c) I – III – IV – II
d) I – II – III – IV
Q.4 The drug Lomustine is mainly used for the treatment of?
a) Primary brain tumors
b) Metastatic brain tumors
c) Colon cancers
d) All of the above
Q.5 Match the drugs with the correct classification.
i. Cytarabine | A. Folate antagonist |
ii. Methotrexate | B. Nitrosoureas |
iii. Lomustine | C. pyrimidine antagonist |
iv. Mechlorethamine | D. Nitrogen mustard |
a) i-A, ii-C, iii-B, iv-D
b) i-D, ii-B, iii-A, iv-C
c) i-C, ii-A, iii-B, iv-D
d) i-B, ii-D, iii-C, iv-A
Q.6 How many statements below are true with respect to the side effects of the drug Lomustine?
a) 1
b) 2
c) 3
d) 4
Q.7 The type of ring system found in Lomustineis?
a) Cyclohexyl ring system
b) Aromatic ring system
c) Benzimidazol ring system
d) Both a) and c)
Answers
1-b
2-d
3-a
4-d
5-c
6-b
7-a
References
[1] Weiss RB, Issell BF. The nitrosoureas: carmustine (BCNU) and lomustine (CCNU). Cancer treatment reviews. 1982 Dec 1;9(4):313-30. [2] Pfreundschuh MG, Schoppe WD, Fuchs R, Pflüger KH, Loeffler M, Diehl V. Lomustine, etoposide, vindesine, and dexamethasone (CEVD) in Hodgkin’s lymphoma refractory to cyclophosphamide, vincristine, procarbazine, and prednisone (COPP) and doxorubicin, bleomycin, vinblastine, and dacarbazine (ABVD): a multicenter trial of the German Hodgkin Study Group. Cancer treatment reports. 1987 Dec;71(12):1203-7.The post LOMUSTINE Synthesis, SAR, MCQ,Chemical Structure and Therapeutic Uses appeared first on Gpatindia: Pharmacy Jobs, Admissions, Scholarships, Conference,Grants, Exam Alerts.
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