Download Tutorial - 2: Anti-cancer agents: Antimetabolites, Antibiotics, Plant

Medicinal Chemistry-III, Tutorial - 2
Medicinal Chemistry – III
Tutorial – 2 (Home Work)
Anti-cancer Agents: Antimetabolites, Antibiotics, Plant alkaloids, and others
1. What are antimetabolite anticancer drug? Classify antimetabolite anticancer drugs and give
two (2) examples of each class.
2. Write the mechanism of action of Methotrexate and 5-Fluorouracil.
3. Write the mechanism of action, uses and side effects of one DNA polymerase/ DNA chain
elongation inhibitors as an anticancer agent.
4. The anti-cancer drug 6-mercaptopurine is rapidly metabolized in the liver by xanthene
oxidase (XO) enzyme into the inactive metabolite (6-thiouric acid). Briefly explain on how
to prevent the inactivation of 6-mercaptopurine by xanthene oxidase (XO) enzyme and
comment on the dosage adjustment of 6-mercaptopurine.
5. Fill-up the blanks based on the following scheme of mechanism of action of anti-cancer
drug: Azathioprine, 6-Mercaptopurine, 6-Thioguanine.
A. The enzyme ____________________________________________ is responsible for
the conversion of anti-cancer drug 6-Mercaptopurine into its thio inosine
monophosphate (TIMP) derivative which can inhibit the first step of
_____________________ biosynthesis. The 6-Mercaptopurine is metabolised by the
enzyme _______________________________ into inactive metabolite 6-thiouric acid
which
can
be
inhibited
by
co-administration
of
another
drug
________________________________.
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Medicinal Chemistry-III, Tutorial - 2
6. Write the mechanism of action and uses of Doxorubicin.
7. Briefly explain the mechanism of action of Vinka alkaloids as anti-cancer agents.
Write the uses of vincristine and vinblastine.
8. Briefly explain the mechanism of action of Paclitaxel (Taxol) as an anti-cancer
agent. Write the uses and side effects of Paclitaxel (Taxol).
9. Write the name and uses of one synthetic and semisynthetic derivatives of
podophyllotoxin. Briefly explain their mechanism of action.
10. Write the mechanism of action, uses and side effects of irinotecan.
11. What is adjuvant and neo-adjuvant chemotherapy? Briefly explain.
12. Briefly explain the mechanism of action and use of Gifitinib.
13. Briefly explain the mechanism of action and use of Trastuzumab.
14. Which of the following drugs is an inhibitor of Dihydrofolatereductase (DHFR)?
a. Cisplatin
b. 5-Fluorouracil
c. Methotrexate
d. 6-Mercaptopurine
15. Which of the following enzymes is inhibited by the anti-cancer drug 5-Fluorouracil?
a. Prunase
b. Dihydrofolate reductase (DHFR)
c. Thymidylate synthetase
d. Serine hydroxymethyl transferase
16. Methotrexate belongs to which of the following class of antimetabolite anti-cancer
drugs?
a. Purine Antagonists
b. Pyrimidine Antagonists
c. DNA Polymerase/ DNA Chain Elongation Inhibitors
d. Miscellaneous Antimetabolite
17. Which of the following enzymes is responsible for the conversion of dUMP to
dTMP?
a. Prunase
b. Dihydrofolate reductase (DHFR)
c. Thymidylate synthetase
d. Serine hydroxymethyl transferase
18. Which of the following statement is TURE regarding the 6-Mercaptopurine??
a. It is a prodrug of azathioprine.
b. Activated by the enzyme thiopurine S-methyltransferase(TPMT).
c. Activated by the enzyme HGPRT.
d. It's half-life decreased if co-administered with allopurinol.
19. Which of the following anti-cancer agent is a Topoisomerase-I inhibitor?
a. Etoposide
b. Topotecan
c. Pentostatin
d. 6-Mercaptopurine
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Medicinal Chemistry-III, Tutorial - 2
20. Which of the following anti-cancer agent is a Topoisomerase-II inhibitor?
a. Etoposide
b. Topotecan
c. Pentostatin
d. 6-Mercaptopurine
21. Which of the following anti-cancer drug cab be isolated from soil bacteria?
a. Actinomycin D
b. Carboplatin
c. Topotecan
d. Mitomycin C
22. Which of the following statements are TRUE for the anti-cancer agents – Paclitaxel
23.
24.
25.
26.
27.
(Taxol)?
a. It blocks the formation of mitotic spindle
b. It inhibit tubulin depolymerisation.
c. It binds to α-subunit of tubulin.
d. It does not stabilises microtubules.
Which of the following anti-cancer drug can block the formation of mitotic spindle?
a. Docetaxel
b. Mitomycin
c. Vincristine
d. Taxol
Which of the following type of chemotherapy is given after surgery or radiation?
a. Adjuvant chemotherapy
b. Neoadjuvant chemotherapy
c. Target based chemotherapy
d. Immunotherapy
Which of the following drug is an example of EGFR tyrosine kinase inhibitor?
a. Actinomycin D
b. Carboplatin
c. Gefitinib
d. Trastuzumab
Which of the following monoclonal antibody is a HER-2 inhibitor?
a. Actinomycin D
b. Carboplatin
c. Gefitinib
d. Trastuzumab
Which of the following cancer is mainly found to be associated with 15-30% the
over-expression of HER-2 oncogene?
a. Breast cancers
b. Cirvical cancer
c. Lung cancer
d. Prostate cancer
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