Cancer Overview and Antineoplastic Agents

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Questions and Answers

What is the primary mechanism of action of Fluorouracil?

Irreversible inhibition of thymidylate synthase (correct)

Interferes with RNA synthesis

Inhibits DNA polymerase

Inhibits dihydrofolate reductase

What type of drug is Tegafur considered?

An active metabolite

An anthracycline antibiotic

A pyrimidine analogue prodrug (correct)

An antifolate drug

How does Cytarabine exert its pharmacological effect?

By converting to cytosine arabinoside triphosphate (correct)

By directly inhibiting thymidylate synthase

By blocking the action of dihydrofolate reductase

By intercalating with DNA

Which compound is particularly toxic to insulin-producing beta cells of the pancreas?

Streptozotocin Signup and view all the answers

What is the function of dihydrofolate reductase in cellular processes?

Convert dihydrofolate to tetrahydrofolate Signup and view all the answers

What distinguishes Temozolomide from Mitozolomide?

Temozolomide is a less toxic analogue of Mitozolomide. Signup and view all the answers

Which drug is noted for treating autoimmune diseases as well as cancer?

Methotrexate Signup and view all the answers

Which mechanism of action is associated with Procarbazine?

Alkylating action through free radical reactions Signup and view all the answers

What is a primary adverse effect associated with anthracycline antibiotics?

Cardiotoxicity Signup and view all the answers

What type of agent does Dacarbazine represent in cancer treatment?

Non-classical alkylating agent Signup and view all the answers

How do alkylating-like agents damage DNA despite lacking alkyl groups?

By forming covalent bonds with DNA Signup and view all the answers

Which of the following drugs inhibits both thymidylate synthase and glycinamide ribonucleotide formyltransferase?

Pemetrexed Signup and view all the answers

What mechanism allows anthracyclines to interfere with DNA replication?

Intercalation between base pairs Signup and view all the answers

Which drug is indicated for the treatment of malignant melanoma?

Dacarbazine Signup and view all the answers

What is a unique characteristic of Lomustine/CCNU in treating brain cancer?

It can cross the blood-brain barrier. Signup and view all the answers

What chemical transformation leads to the formation of the active alkylating agent from Dacarbazine?

Demethylation and conversion to diazomethane Signup and view all the answers

What effect does increasing the length of the side chain beyond 2 C-atoms have on antineoplastic activity?

It gives no antineoplastic activity. Signup and view all the answers

How does the nature of the group (R) attached to nitrogen in nitrogen mustards affect chemical reactivity?

It is the prime determinant of chemical reactivity. Signup and view all the answers

What is the primary mechanism through which alkylsulphonate derivatives, such as Busulfan, operate?

By attacking the carbon adjacent to the mesylate group. Signup and view all the answers

What is the main characteristic of aryl (aromatic) nitrogen mustards compared to aliphatic nitrogen mustards?

They stabilize the lone pair of electrons through resonance. Signup and view all the answers

What type of cancers is Thiotepa primarily used to treat?

Breast, ovarian, and bronchogenic carcinomas. Signup and view all the answers

Which compound undergoes decomposition to produce alkyl diazohydroxide leading to DNA alkylation?

Carmustine. Signup and view all the answers

What role does the aziridinium ion play in the mechanism of action for nitrogen mustards?

It facilitates the alkylation of DNA. Signup and view all the answers

What is the primary chemical feature that distinguishes nitrosoureas from other chemotherapeutic agents?

Inclusion of a nitroso group and a urea. Signup and view all the answers

What is the primary mechanism by which platinum-based chemotherapeutic drugs like Cisplatin interfere with cell division?

They form crosslinks with DNA. Signup and view all the answers

Which of the following is a characteristic of Carboplatin compared to Cisplatin?

It has reduced side effects. Signup and view all the answers

Which of the following statements is true regarding Oxaliplatin?

It is often combined with other drugs like Fluorouracil and Folinic acid. Signup and view all the answers

What is the role of antimetabolites in cancer chemotherapy?

They inhibit the use of specific metabolites. Signup and view all the answers

Which class of drugs includes compounds like 6-Mercaptopurine and Thioguanine?

Antimetabolite agents. Signup and view all the answers

What enzyme do purine analogues primarily compete with for inhibition?

Hypoxanthine-guanine phosphoribosyl transferase. Signup and view all the answers

What happens to the chloride ligands in Cisplatin during its activation process in the body?

They are slowly replaced by water molecules. Signup and view all the answers

Which combination is commonly referred to as FOLFOX in colorectal cancer treatment?

Fluorouracil, Folinic acid, and Oxaliplatin. Signup and view all the answers

What is the effect of having an (R) configuration at the chiral carbon in the E-ring?

It renders the compound inactive. Signup and view all the answers

Which of the following modifications at position 12 and 14 leads to a specific outcome?

Formation of inactive derivatives. Signup and view all the answers

What distinguishes topoisomerase II poisons from catalytic inhibitors?

Poisons enhance enzyme binding to DNA, inhibitors block enzyme activity. Signup and view all the answers

Which of the following statements about Vinca alkaloids is correct?

They inhibit tubulin assembly into microtubules. Signup and view all the answers

What is one of the adverse effects associated with Teniposide?

Severe myelosuppression. Signup and view all the answers

How does the enhancement of the lactone ring affect activity?

Enhances the activity. Signup and view all the answers

Which characteristic is true for microtubules?

They undergo constant assembly and disassembly. Signup and view all the answers

What is the FDA approval date of Topotecan as a topoisomerase I inhibitor for oral use?

October 15, 2007. Signup and view all the answers

What is the primary characteristic of cancer cells compared to normal cells?

Cancer cells divide and grow uncontrollably. Signup and view all the answers

Which of the following is NOT a common type of cancer in males?

Breast cancer Signup and view all the answers

What challenge must cancer chemotherapy overcome?

Minimize harm to normal cells while killing all cancer cells. Signup and view all the answers

What is the mechanism of action for alkylating agents?

They attach an alkyl group to DNA. Signup and view all the answers

Which of the following factors is NOT known to increase the risk of developing cancer?

Healthy diet Signup and view all the answers

What type of antineoplastic agent is nitrogen mustard classified as?

Classical Alkylating agent Signup and view all the answers

Cancer treatment strategies generally seek to achieve which of the following outcomes?

To kill all cancer cells with minimal harm to normal cells. Signup and view all the answers

How prevalent was cancer in the year 2015, according to recent statistics?

Around 90.5 million people had cancer. Signup and view all the answers

Study Notes

Cancer

Cancer is a broad group of diseases involving unregulated cell growth, forming malignant tumors, and invading nearby parts.
Causes of cancer are diverse, complex, and not fully understood. Factors increasing cancer risk include tobacco use, diet, infections, radiation, inactivity, obesity, and genetics.
Cancer risk generally increases with age.
In 2015, 90.5 million people had cancer, and in 2018, 18.1 million new cases were diagnosed. Cancer caused about 9.6 million deaths in 2018.
Common cancers in males include lung, prostate, colorectal, and stomach cancers.
Common cancers in females include breast, colorectal, lung, and cervical cancers.

Rationale of Antineoplastic Agents

Cancer cells multiply at a faster rate than normal cells.
Obstacles of cancer chemotherapy include selectivity, killing all cancer cells, and minimizing harm to normal cells.

Classification of Anticancer Agents

Alkylating agents
- Attach an alkyl group to DNA (guanine base)
- Cancer cells are more sensitive to DNA damage
- Many are also carcinogenic.
- Classical alkylating agents:
Nitrogen mustard: similar to mustard gas, used medicinally and in warfare
Antimetabolites:
- Compete or mimic metabolic pathways to prevent cell function by interfering with DNA and RNA synthesis
- Common analogy examples are purine and pyrimidine analogues
Antibiotics:
- Some antibiotics demonstrate anti-cancer activity.
Natural products:
- Include natural compounds with anticancer activity.
Protein kinase inhibitors:
- Target specific kinases involved in cell signaling pathways
Hormone-based Therapy:
- Target hormone-dependent cancers like breast, endometrial, and prostate cancers.

Mechanism of Action (Specific Examples)

Cyclophosphamide (Endoxan®): A prodrug activated by enzymes; the active metabolite causes DNA damage.
Mechlorethamine: Transfer alkyl group to cellular constituents, leading to cellular lethality.
Streptozotocin: Specifically toxic to insulin-producing beta cells in the pancreas.
Dacarbazine: Bioactivated by liver enzymes to form an alkylating agent, causing DNA damage.
Mitozolomide / Temozolomide: Produce diazomethane to cause DNA damage.
Procarbazine: Is oxidized to methyldiazine, resulting in alkylation (DNA damage).
Platinum-based chemotherapeutic drugs (cisplatin, carboplatin, oxaliplatin): Damage DNA, disrupt cell division, usually by forming crosslinks in DNA.
Topoisomerase I Inhibitors (Camptothecin, Topotecan, Irinotecan): Prevent relaxation of supercoiled DNA, leading to DNA damage and cell death
Topoisomerase II Inhibitors (Teniposide): Inhibit DNA synthesis by blocking topoisomerase activity.
Anthracycline antibiotics (daunorubicin, doxorubicin, idarubicin): Intercalate in DNA, inhibiting DNA replication and causing DNA damage.
Actinomycin D: Binds to DNA and interferes with its function and replication.
Mitomycin: Crosslinks DNA
Vinca Alkaloids (vincristine, vinorelbine): Inhibit microtubule assembly, crucial for cell division
Taxanes (paclitaxel): Stabilize microtubules, preventing cell division.
Protein Kinase Inhibitors (Gefitinib, Imatinib): Inhibit specific kinases implicated in cancer cell growth pathways.
Hormone-based therapies (estrogens, progestins, androgens, LHRH agonists, antiestrogens, antiandrogens): Affect hormone-dependent cancers by either inhibiting or acting as competitors for hormones. Aromatase inhibitors (Aminoglutethimide, anastrozole, letrozole) block estrogen production in breast cancer.

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Description

This quiz explores the fundamentals of cancer, including its causes, statistics, and common types. Furthermore, it provides insight into the rationale and classification of antineoplastic agents, essential for understanding cancer treatment. Test your knowledge on cancer and its treatment methods!