Medicinal Chemistry Ch 9 Test Bank
Questions All Answered Correct Rated
A+.
Doxorubicin - Answer Intercalating agent:
- Intercalates with major groove of helix
- **Prevents activity of topoisomerase II by stabilizing DNA-enzyme complex**
- (+)NH3 interacts with charged phosphate groups
MOA of topoisomerase II - Answer Relieves strain by cleaving DNA chain, forming a transient
double-stranded break, and passing intact strand through transient double-stranded break
1) **Tyr residues in enzyme are involved in chain-breaking process; transient formation of ester
bond btwn Tyr and DNA molecule**
2) After Tyr interaction, enzyme pulls chains apart to create gap
3) Intact strand passed through gap and break is resealed
A) Anthracyclines
B) 3 - Answer The following group of structures are intercalating anticancer agents. To which
family of compounds do these structures belong? How many rings of the tetracyclic system are
involved in intercalation?
Proflavine - Answer Intercalating agent:
- Intercalates with minor groove
- planar tricyclic system slips through base-pair layers
- (+)NH3 interacts with charged phosphate groups in DNA to stabilize intercalation
Proflavine is an intercalating agent which was used to treat wounded soldiers in the
, b. Its planar shape is important to intercalation.
c. The primary amine groups are protonated and interact with phosphate groups of the DNA
backbone.
d. When inserted into DNA, the tricyclic system can form van der Waals interactions with base
pairs above and below it. - Answer a - too toxic for systemic use; may be used topically or for
superficial wounds
Dactinomycin is an intercalating agent. Which
region of the molecule is chiefly responsible for its ability to intercalate into DNA? MOA? -
Answer A) tricyclic system
B) Prevents unwinding of DNA and RNA polymerase from catalyzing the synthesis of mRNA
Dactinomycin is an intercalating anticancer agent. Which region of the molecule
interacts with the sugar phosphate backbone of DNA? - Answer The cyclic peptides
The cyclic peptides have polar functional groups which can interact with the polar phosphate
groups of the sugar phosphate chain.
What term is used to describe the strategy where an oligonucleotide is designed such that it
base pairs with a segment of messenger RNA and blocks protein translation?
a. Sense therapy.
b. Anticodon therapy.
c. Codon therapy.
d. Antisense therapy - Answer d
Deoxythymidine - Answer
Deoxyguanosine - Answer
Deoxyadenosine - Answer
Deoxycytidine - Answer
Questions All Answered Correct Rated
A+.
Doxorubicin - Answer Intercalating agent:
- Intercalates with major groove of helix
- **Prevents activity of topoisomerase II by stabilizing DNA-enzyme complex**
- (+)NH3 interacts with charged phosphate groups
MOA of topoisomerase II - Answer Relieves strain by cleaving DNA chain, forming a transient
double-stranded break, and passing intact strand through transient double-stranded break
1) **Tyr residues in enzyme are involved in chain-breaking process; transient formation of ester
bond btwn Tyr and DNA molecule**
2) After Tyr interaction, enzyme pulls chains apart to create gap
3) Intact strand passed through gap and break is resealed
A) Anthracyclines
B) 3 - Answer The following group of structures are intercalating anticancer agents. To which
family of compounds do these structures belong? How many rings of the tetracyclic system are
involved in intercalation?
Proflavine - Answer Intercalating agent:
- Intercalates with minor groove
- planar tricyclic system slips through base-pair layers
- (+)NH3 interacts with charged phosphate groups in DNA to stabilize intercalation
Proflavine is an intercalating agent which was used to treat wounded soldiers in the
, b. Its planar shape is important to intercalation.
c. The primary amine groups are protonated and interact with phosphate groups of the DNA
backbone.
d. When inserted into DNA, the tricyclic system can form van der Waals interactions with base
pairs above and below it. - Answer a - too toxic for systemic use; may be used topically or for
superficial wounds
Dactinomycin is an intercalating agent. Which
region of the molecule is chiefly responsible for its ability to intercalate into DNA? MOA? -
Answer A) tricyclic system
B) Prevents unwinding of DNA and RNA polymerase from catalyzing the synthesis of mRNA
Dactinomycin is an intercalating anticancer agent. Which region of the molecule
interacts with the sugar phosphate backbone of DNA? - Answer The cyclic peptides
The cyclic peptides have polar functional groups which can interact with the polar phosphate
groups of the sugar phosphate chain.
What term is used to describe the strategy where an oligonucleotide is designed such that it
base pairs with a segment of messenger RNA and blocks protein translation?
a. Sense therapy.
b. Anticodon therapy.
c. Codon therapy.
d. Antisense therapy - Answer d
Deoxythymidine - Answer
Deoxyguanosine - Answer
Deoxyadenosine - Answer
Deoxycytidine - Answer
