Download Tutorial - 1: Anti-cancer agents: Introduction, Alkylating and

Medicinal Chemistry-III, Tutorial - 1
Medicinal Chemistry – III
Tutorial -1 (Home Work)
Anti-cancer agents: Introduction, Alkylating and Metallating Agents
1) Which of the following statements regarding carcinoma is correct?
a. It is a tumor of epithalial cell.
b. It is a tumor of bone marrow.
c. It is a tumor of muscle.
d. It is a tumor of blood cell.
2) Which of the following cancer is caused by Human papiloma virus?
a. Cervical cancer
b. Liver cancer
c. Lung cancer
d. Breast cancer
3) Which of the following type of mutation can pass to off springs?
a. Germline mutation
b. Somatic mutation
c. Acquired mutation
d. Genetic mutation
4) Which of the following treatment strategy can provide greatest chance of cure for cancer?
a. Surgery
b. Chemotherapy
c. Immunotherapy
d. Radiation therapy
5) Which of the following type of cancer is caused by Epstein-Barr virus?
a. Cervical cancer
b. Liver cancer
c. Burkit's lymphoma
d. Breast cancer
6) Which of the following statement regarding Myeloma is CORRECT?
a. It is a tumor of epithalial cell.
b. It is a tumor of bone marrow.
c. It is a tumor of blood cell.
d. It is a tumor of white blood cells that produces antibodies.
7) Which of the following statement is FALSE regarding alkylating anti-cancer agents?
a. It prevents the replication of DNA.
b. It can cause both inter-strand and intra-strand cross-linking of DNA.
c. It can only cause intra-strand cross-linking of DNA.
d. Alkylation of nucleic acid bases can result in miscoding.
8) How the anti-cancer agent chlormethaine can act as a highly reactive alkylating agent to bind a DNA?
a. By forming aziridinium ion.
b. By forming a zwiter ion.
c. By forming an anion.
d. By forming methyldiazonium ion.
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Medicinal Chemistry-III, Tutorial - 1
9) In which of the following form guanine causes abnormal base pairing with other nucleotide of DNA after
binding with an anti-cancer alkylating agent?
a. By forming keto tautomer.
b. By forming enol tautomer.
c. By forming both keto and enol tautomers.
d. By forming cation.
10) Which of the following agent can be used for the treatment of extravasation?
a. 0.16 M sodium carbonate
b. 0.16 M sodium sulfate
c. 0.16 M sodium thiosulfate
d. 0.16 M sodium chloride
11) Which of the following anticancer agent can cause faster rate of alkylation of DNA?
a. Chlorambucil
b. Mechlorethamine
c. Sulfur mustard
12) Which of the following anti-cancer alkylating agent is an example of prodrug?
a. Cisplatin
b. Estramustine
c. Chlormethine
d. Chlorambucil
13) What is the name of the toxic metabolite of cyclophosphamide responsible for hemorrhagic cystitis?
a. Acrolein
b. Methyl hydrazine
c. Methyl diazonium ion
d. Cyclopentane
14) Which of the following anti-cancer alkylating agent can cause hyperuricemia?
a. Busulfan
b. Carmustine
c. Chlorambucil
d. Ifosfamide
15) Which of the following alkylating agent contains Nitrosourea functional group?
a. Carmustine
b. Cyclophosphamide
c. Chlorambucil
d. Busulfan
16) The co-administration of which of the following agent can avoid the acrolein toxicity of Ifosfamide?
a. Carmustine
b. cyclophosphamide
c. N-acetylcysteine
d. Sodium thiosulphate
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Medicinal Chemistry-III, Tutorial - 1
17) Which of the following drug can cause free radical methylation of DNA?
a. Busulfan
b. Lomustine
c. Procarbazine
d. Thiotepa
18) Which of the following anti-cancer alkylating agent contains sulfonate leaving group?
a. Busulfan
b. Carmustine
c. Procarbazine
d. Thiotepa
19) Which of the following nucleotide of DNA is preferred for binding by Cisplatin?
a. Adenine
b. Cytosine
c. Guanine
d. Thymine
20) Which of the following metallating anti-cancer agent has less toxicity?
a. Cisplatin
b. Mitomycin
c. Carboplatin
d. Dacarbazine
21) Which of the following anti-cancer agent can be used for the treatment of prostate cancer?
a. Carmustine
b. Chlormethine
c. Estramustine
d. 6-Mercaptopurine
22) Which of the following anticancer agent can be used for the palliative treatment of brain tumors?
a. Carmustine
b. Cyclophosphamide
c. Melphalan
d. Thiotepa
23) Which of the extravasation process can cause severe and long lasting tissue injury?
a. Vesicant
b. Irritants
c. Myelosuppression
d. Neutropenia
24) Which of the following statements are FALSE for cancer chemotherapy?
I.
II.
III.
IV.
It is the use of medicines or drugs along with radiation to treat cancer.
It provides maximum chance of cure as compared to other cancer therapy.
It always provides specific treatment and attacks only cancer cells.
They cause extravasation if given by oral administration.
A.
B.
C.
D.
E.
I and II only
II, and III only
I, II and III only
II, III and IV only
I, II, III and IV
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Medicinal Chemistry-III, Tutorial - 1
25) Answer the following questions either TRUE (T) or FALSE (F).
A. The anti-cancer drug Thiotepa belongs to a class of aziridine-alkylating agents.
B. The anti-cancer drug Carmustine (belonging to the class of nitrosourea-alkylating agents) is highly vesicant
and cannot cross blood brain barrier (BBB).
C. Extravasation effect of any anti-cancer drug can be increased by the application of 0.16M sodium
thiosulfate.
D. A drug is known as vesicant, if its extravasation effect is self-limiting.
E. Somatic mutations are mutations that is not inherited by offspring.
26) What is extravasation effect of chemotherapy? Classify extravasation effects and give one example each.
27) Write the name, structure, use, side effects and mechanism of action of any one anticancer alkylating agents.
28) What is the advantage of Uracil mustard over nitrogen mustard as an anticancer alkylating agent?
29) What is the advantage of Melphalan over Chlorambucil as an anticancer alkylating agent?
Cl
NH2
HOOC
HOOC
Cl
N
N
H
Cl
Cl
Melphalan
Chlorambucil
30) Write the name, structures uses and mechanism of action of two (2) alkylating anticancer agents containing
nitrosourea functional group.
31) Write the name, structure and uses of one (1) platinum containing anticancer agent.
32) Write the synthesis, uses and side effects of cyclophosphamide.
33) Write the name, structure, uses, side effects and mechanism of actions of one (1) alkylating anticancer agent
containing aziridine functional group.
34) Write the name, uses, side effects and mechanism of actions of two (2) alkylating anticancer agents containing
methylhydrazine functional group.
35) Which of the following drug is considered as less reactive anticancer alkylating agents? Give reason.
Cl
Cl
N
Cl
Mechlorethamine
CH3
COOH
N
Cl
Chlorambucil
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