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PY3 > Oncology: DNA Alkylating Agents Lapinsky > Flashcards

Oncology: DNA Alkylating Agents Lapinsky Flashcards

1
Q

What are DNA Alkylating agents classified as?

A

CCNS drugs

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2
Q

DNA alkylating agents are capable of introducing alkyl groups onto what sites within biological macromolecules?

A

Nucleophilic

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3
Q

DNA alkylating agents tend to work according to the…

A

Rate therapy of cancer chemotherapy

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4
Q

What are cancer cells more sensitive to?

A

DNA damage via alkylation of DNA

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5
Q

DNA alkylating agents as anti-cancer drugs are

A

Highly reactive

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6
Q

What ion do DNA Alkylating contain that has a partial of a full positive charge? Which agents have this ion?

A

Aziridinium ion; Nitrogen Mustards

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7
Q

What kind of compounds are DNA alkylating agents?

A

Electrophiles

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8
Q

DNA alkylating agents contain a good ________. What ion is it?

A

Leaving group; Cl-

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9
Q

What is the desired target of the DNA alkylating agents?

A

DNA

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10
Q

What are undesired targets of DNA alkylating agents?

A

Protein and enzymes

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11
Q

What happens if DNA alkylating agents bind to their undesired drug targets?

A

More likely to have long lasting ADRs

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12
Q

What is the single most important nucleophile for the alkylating agents to bind to?

A

The N7 atom of guanine

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13
Q

What 2 things can cause the alkylating agents to have some the worst long lasting adverse side effects?

A
  1. Formation of covalent, irreversible drug
  2. Lack of drug target and cell selectivity
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14
Q

ALL DNA alkylating agents are potentially what 2 things?

A

Mutagenic and carcinogenic

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15
Q

The shift from KETO tautomer of guanine to the ENOL tautomer of alkylated Guanine leads alkylated guanine to do what?

A

Abnormally base pair with thymine instead of cytosine

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16
Q

DNA mutations resulting from the alkylation of DNA by a DNA alkylating agent could potentially lead to what 3 things?

A
  1. Cell apoptosis
  2. An irreversible state of cell dormancy
  3. Conversion of a normal healthy cell into a cancer cell
17
Q

What is it called when a cell goes into irreversible dormancy?

A

Cell senescence

18
Q

Alkylated DNA within cancer cells acts as a ________ to induce cell apoptosis

A

Chemical signal

19
Q

What functional group mimics a purine for DNA and RNA synthesis in Bendamustine?

A

Benzimidazole ring

20
Q

What is the natural amino acid in Melphalan?

A

L- phenylalanine

21
Q

What are the 2 nitrogen mustards?

A
  1. Melphalan
  2. Bendamustine
22
Q

Since cancer cells spend less time in the resting phases than normal cells, cancer cells are more likely to be?

A

More metabolically active

23
Q

Original prototype nitrogen mustard

A

Mechlorethamine

24
Q

When cancer cells are tricked into taking up the DNA alkylating agents more than the normal cells

A

Preferential killing

PY3 (24 decks)

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