Cancer Chemotherapeutic Agents Lecture 1 Dr M. Casely-Hayford, PhD
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Questions and Answers

What is the term used to describe the process where cancer cells invade other parts of the body and set up secondary tumors?

  • Neoplasm
  • Malignant
  • Alkylation
  • Metastasis (correct)

    • Which disease caused a quarter of all deaths in 2000 according to the WHO?

  • Diabetes
  • Stroke
  • Cancer (correct)
  • Heart disease

    • What is the term used to describe new growth and is considered a more accurate term for cancer?

  • Metastasis
  • Carcinoma
  • Neoplasm (correct)
  • Tumor

    • What is the characteristic of cancer cells that distinguishes them from normal cells?

    <p>Loss of differentiation</p> Signup and view all the answers

    What is the term used to describe a local swelling, often caused by cancer?

    <p>Tumor</p> Signup and view all the answers

    What regulatory mechanisms do cancer cells lose that lead to uncontrolled growth and multiplication?

    <p>Cell cycle checkpoints</p> Signup and view all the answers

    Which of the following is NOT a common cause of genetic mutations that can lead to cancer?

    <p>Sunlight exposure</p> Signup and view all the answers

    Which type of agents acts directly on existing DNA to selectively destroy a tumor or limit its growth?

    <p>Drugs that inhibit DNA synthesis</p> Signup and view all the answers

    Which type of DNA interactive agents can form cross-links between two complementary DNA strands?

    <p>Alkylating and methylating agents</p> Signup and view all the answers

    Which of the following is NOT a characteristic of cancer?

    <p>Increased cellular differentiation</p> Signup and view all the answers

    Which type of agents interferes with DNA replication by forming bridges within a single DNA strand?

    <p>Bifunctional agents</p> Signup and view all the answers

    Which of the following is NOT a type of DNA interactive agents that are used in cancer chemotherapy?

    <p>Drugs targeting cellular metabolism</p> Signup and view all the answers

    Which of the following is NOT a common event leading to the accumulation of mutations in oncogenes and tumor suppressor genes?

    <p>Transcriptional errors</p> Signup and view all the answers

    Which of the following is the most significant cause of cancer deaths?

    <p>Metastases</p> Signup and view all the answers

    Which type of drugs is the most widely used group in the clinical practice of cancer chemotherapy?

    <p>DNA interactive agents</p> Signup and view all the answers

    Which of the following is NOT a common cause of genetic mutations that can lead to cancer?

    <p>Aging</p> Signup and view all the answers

    What is the primary cause of mispairing of nucleotides due to alkylation?

    <p>The displacement of tautomeric equilibrium to the more stable enol form</p> Signup and view all the answers

    Which type of alkylation agent can form bridges within a single DNA strand?

    <p>Bi-functional agents</p> Signup and view all the answers

    What is the primary mechanism of cytotoxicity induced by alkylation agents?

    <p>Induction of mispairing of nucleotides</p> Signup and view all the answers

    What is the result of tautomeric equilibrium being displaced to the more stable enol form in alkylated G?

    <p>H-bonding with cytosine is weakened</p> Signup and view all the answers

    What is the primary cause for the cytotoxicity of bi-functional agents?

    <p>Formation of bridges between two complementary DNA strands</p> Signup and view all the answers

    What is the primary cause of DNA fragmentation by hydrolytic reactions and by the action of repair enzymes?

    <p>The attempt of repair enzymes to excise alkylated bases</p> Signup and view all the answers

    What is the main reason why bifunctional alkylating agents are considered more cytotoxic than monofunctional ones?

    <p>There is a direct correlation between the degree of interstrand cross-linking and cytotoxicity</p> Signup and view all the answers

    Which of the following types of DNA alkylating agents is known to attack DNA via covalent modification?

    <p>Nitrogen mustards</p> Signup and view all the answers

    Why are DNA crosslinking agents usually more effective than monoalkylators?

    <p>They form interstrand or intrastrand crosslinks</p> Signup and view all the answers

    What is the mechanism of action for chlormethine, an aliphatic nitrogen mustard?

    <p>Anchimeric assistance from the nitrogen atom forming aziridinium cation</p> Signup and view all the answers

    Which form of cancer is particularly rich in GC-sequences and susceptible to alkylating/crosslinking agents?

    <p>Burkitt's lymphoma</p> Signup and view all the answers

    What was the effect of exposure to the chemical warfare agent sulphur mustard during the war?

    <p>Lowered white blood cell count</p> Signup and view all the answers

    'Mustard gas' developed from war gas has a high chemical reactivity towards which biological molecules?

    <p>DNA nucleophilic centres</p> Signup and view all the answers

    'Local extravasation usually causes tissue necrosis' refers to what specific compound used in chemotherapy regimens?

    <p>'Chlormethine'</p> Signup and view all the answers

    'Attempts made to reduce side effects' of what compound due to its high reactivity and toxicity?

    <p>'Chlorambucil'</p> Signup and view all the answers

    What is the primary approach used to reduce the reactivity of certain drugs before they reach their site of action?

    <p>Reducing the nucleophilic character of the tertiary nitrogen by attaching it to electron-withdrawing aromatic rings</p> Signup and view all the answers

    What is the role of the P=O group in the structure of cyclophosphamide?

    <p>Decreases the electrophilicity of the nitrogen</p> Signup and view all the answers

    What is the primary complication caused by acrolein, a potent electrophilic by-product of cyclophosphamide metabolism?

    <p>Hemorrhagic cystitis</p> Signup and view all the answers

    Which agent is given as an adjuvant to protect the bladder and kidney during cyclophosphamide treatment?

    <p>Mesna</p> Signup and view all the answers

    What are the two major metabolites produced by further enzymatic oxidation of aldophosphamide?

    <p>4-ketocyclophosphamide and carboxyphosphamide</p> Signup and view all the answers

    What is the mechanism by which Mesna reacts with acrolein?

    <p>Michael addition</p> Signup and view all the answers

    How do the active cross-linking agents produced by cyclophosphamide metabolism interfere with DNA processing?

    <p>By blocking DNA replication and transcription</p> Signup and view all the answers

    What is the primary effect of alkylation by cyclophosphamide metabolites on DNA replication and RNA transcription?

    <p>Blocking of DNA replication and RNA transcription</p> Signup and view all the answers

    What is the primary mechanism by which cyclophosphamide is activated in vivo?

    <p>Cytochrome P-450-dependent metabolic activation in the liver</p> Signup and view all the answers

    What is the primary goal of attaching the tertiary nitrogen to electron-withdrawing aromatic rings in the design of certain drugs?

    <p>To decrease reactivity</p> Signup and view all the answers

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