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cancer chemotherapy Flashcards

1
Q

The nitrogen mustards (Alkylating agents) contain highly electrophilic groups and form covalent bonds to nucleophilic groups in DNA. true or false?

A

true

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2
Q

alkylating agents are useful anti‐tumour agents that prevent replication and transcription. true or false?

A

true

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3
Q

alkylation of nucleic acid bases can result in miscoding. TRUE OR FALSE?

A

TRUE

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4
Q

what are the toxic side effects of alkylating agents?

A

alkylation of proteins

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5
Q

what does Melphalan mimic?

A

phenylalanine and is transported into cells by normal transport proteins

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6
Q

The uracil ring in uracil mustardis electron withdrawingand so this is a less reactive alkylating agent. true or false?

A

true

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7
Q

what does the uracil ring mimic?

A
  • nucleic acid base

- is concentrated in fast growing cells

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8
Q

what group in estramustine is electron withdrawing?

A

urethane group

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9
Q

what is the most commonly used alkylating agent?

A

Cyclophosphamide

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10
Q

Cyclophosphamide is a non‐toxic prodrug which is orally active. true or false?

A

true

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11
Q

what is the by-producted of the activated Cyclophosphamide by alkylation and what is it associated with?

A

Acrolein

- Associated with toxicity

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12
Q

what is the most clinically toxic anti-cancer drugs?

A
  • Mitomycin C
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13
Q

Mitomycinis also a prodrug activated in vivo to form an alkylating agent. true or false?

A

true

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14
Q

is cisplatin a prodrug?

A
  • yes
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15
Q

when is cisplatin activated?

A

is activated in cells with low chloride ion concentration

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16
Q

cisplatin binds to DNA in regions rich in guanine units. true or false?

17
Q

what kind of strands does cisplatin form that causes localised unwinding of the DNA double helix and inhibits transcription?

A

Intrastrands

18
Q

anthracyclines are what types of agents?

A

Intercalating agents

19
Q

The planar anthraquinone of anthracyclines moiety intercalates between the DNA base pairs and the carbohydrate moiety binds into the minor groove. true or false?

20
Q

5‐Fluorouracil(5‐FU) is a prodrugthat is metabolised to give 5‐F‐dUMP which then acts an inhibitor of thymidylatesynthase. True or false?

21
Q

How does 5‐F‐uDMP inhibits thymidylate synthase?

A
  • The C-F bond is stronger than the C-H bond which is normally cleaved by thymidylatesynthase
  • This causes the enzyme to be inhibited irreversibly
22
Q

Capecitabineis a produgof 5‐fluorouracilwhich is itself a prodrug. true or false?

23
Q

what is the only chemotherapy drug availabe for treatment of pancreatic cancer?

A
  • Gemcitabine
24
Q

Gemcitabine is the fluorinated analogue of 2’‐deoxycytidine and it interacts with DNA and RNA polymerases within the cancerous cell which inhibits nucleic acid replication and repair. TRUE OR FALSE?

25
Q

what are kinases?

A
  • They are enzymes that catalyse phosphorylation
26
Q

overexpression of kinases can lead to cancers. true or false?

27
Q

give examples of type 1 and type 2 kinase inhibitors?

A
  • Type 1 - gefitinib

- type 2 - Imatinib

28
Q

how do type 1 and 2 kinase inhibiotrs work?

A
  • Type 1:
  • bind to the active conformation of the enzyme
  • inhibitors bind to the ATP binding site and block access to ATP
  • Type 2:
  • act on the inactive conformation of the enzyme
  • bind to the enzyme and stabilise the inactive conformation
29
Q

which are more likely to be selective between type 1 and 2 kinase inhibitors?

30
Q

there is a greater risk that random mutation of the target will weaken binding interactions and lead to drug resistance with type 2 kinase inhibiotrs are they are ore selective. true or false?

31
Q

type III inhibitors bind to regions of the active site not occupied by ATP. true or false?

32
Q

the EGF‐receptor of gifitnib is a tyrosine kinase receptor. true or false?

33
Q

how does gefitinib work?

A

It inhibits the kinase active site of the epidermal growth factor receptor

34
Q

gefitinib the morpholine ring increases water solubility. true or false?

35
Q

Imatinib is a selective inhibitor for a hybrid tyrosine kinase (Bcr‐Abl)which is active in certain tumour cells. true or false?

36
Q

what increases the activity, selectivity and water solubility in Imatinib?

A

piperazine

37
Q

list the different types of cancer chemotherapy classes of drugs?

A
  • Alkylating agents
  • Kinase inibitors
  • platinum compounds
  • Mitomycin C
  • Thiopurines
  • inhibitors of thymidylate synthase
  • Intercalating agents
  • Dna polymerases

Tony's lectures (8 decks)

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