[MEDICINAL CHEMISTRY] Antineoplastic , Cell Cycle Specific & Non-specific Agents

b. Pulmonary fibrosis

Bleomycin causes ______

a. Cardiotoxicity
b. Pulmonary fibrosis
c. Nephrotoxicity
d. Peripheral neuropathy

b. Pulmonary fibrosis

Busulfan causes _____

a. Cardiotoxicity

b. Pulmonary fibrosis

c. Nephrotoxicity

d. Peripheral neuropathy

b. Nephrotoxicity and ototoxicity

Cisplatin causes ______

a. Cardiotoxicity and pulmonary fibrosis

b. Nephrotoxicity and ototoxicity

c. Peripheral neuropathy and hepatotoxicity

d. Myelosuppression and alopecia

b. Nephrotoxicity and ototoxicity

Carboplatin causes _____

a. Cardiotoxicity and pulmonary fibrosis

b. Nephrotoxicity and ototoxicity

c. Peripheral neuropathy and hepatotoxicity

d. Myelosuppression and alopecia

c. Cardiotoxicity

Doxorubicin causes _____

a. Nephrotoxicity

b. Ototoxicity

c. Cardiotoxicity

d. Pulmonary fibrosis

b. Myelosuppression

Methotrexate causes ______

a. Cardiotoxicity
b. Myelosuppression
c. Pulmonary fibrosis
d. Nephrotoxicity

b. Myelosuppression

5-Flurouracil causes ______

a. Cardiotoxicity
b. Myelosuppression
c. Pulmonary fibrosis
d. Nephrotoxicity

b. Neurotoxicity (crosses BBB)

Nitrosoureas (lomustine, carmustine) causes _____

a. Cardiotoxicity
b. Neurotoxicity (crosses BBB)
c. Pulmonary fibrosis
d. Nephrotoxicity

b. Neurotoxicity (crosses BBB)

Lomustine causes ____

a. Cardiotoxicity
b. Neurotoxicity (crosses BBB)
c. Pulmonary fibrosis
d. Nephrotoxicity

b. Neurotoxicity (crosses BBB)

Carmustin causes _____

a. Cardiotoxicity
b. Neurotoxicity (crosses BBB)
c. Pulmonary fibrosis
d. Nephrotoxicity

b. Hemorrhagic cystitis

Cyclophosphamide causes ______

a. Pulmonary fibrosis
b. Hemorrhagic cystitis
c. Cardiotoxicity
d. Ototoxicity

c. Peripheral neuropathy

Taxanes (paclitaxel, docetaxel) causes _____

a. Cardiotoxicity
b. Nephrotoxicity
c. Peripheral neuropathy
d. Pulmonary fibrosis

c. Peripheral neuropathy

Paclitaxel causes _____

a. Cardiotoxicity
b. Nephrotoxicity
c. Peripheral neuropathy
d. Pulmonary fibrosis

c. Peripheral neuropathy

Docetaxel causes _____

a. Cardiotoxicity
b. Nephrotoxicity
c. Peripheral neuropathy
d. Pulmonary fibrosis

b. Peripheral neuropathy

Vinca alkaloids (vincristine > vinblastine) causes _____

a. Cardiotoxicity
b. Peripheral neuropathy
c. Nephrotoxicity
d. Hemorrhagic cystitis

b. Peripheral neuropathy

Vincristine causes _____

a. Cardiotoxicity
b. Peripheral neuropathy
c. Nephrotoxicity
d. Hemorrhagic cystitis

b. Peripheral neuropathy

Vinblastine causes _____

a. Cardiotoxicity
b. Peripheral neuropathy
c. Nephrotoxicity
d. Hemorrhagic cystitis

b. Antineoplastic agents

Prevents, inhibits, or halts the development of a neoplasm or tumor.

a. Antibiotics

b. Antineoplastic agents

c. Antivirals

d. Antifungals

b. Benign tumor

Collection of abnormally proliferating cells that does not invade surrounding tissues.

a. Malignant tumor

b. Benign tumor

c. Carcinoma

d. Sarcoma

b. Malignant tumor

Collection of abnormally proliferating cells that invades and metastasizes to all parts of the body.

a. Benign tumor

b. Malignant tumor

c. Adenoma

d. Lipoma

b. Carcinoma

Solid tumor arising from epithelial cells.

a. Sarcoma

b. Carcinoma

c. Lymphoma

d. Leukemia

b. Sarcoma

Solid tumor arising from connective tissues.

a. Carcinoma

b. Sarcoma

c. Lymphoma

d. Leukemia

c. Osteosarcoma

Sarcoma of the bone.

a. Liposarcoma

b. Leiomyosarcoma

c. Osteosarcoma

d. Rhabdomyosarcoma

b. Leiomyosarcoma

Sarcoma of the muscles.

a. Osteosarcoma

b. Leiomyosarcoma

c. Liposarcoma

d. Chondrosarcoma

b. Lymphoma

Hematologic malignancy of the lymphatic system.

a. Leukemia

b. Lymphoma

c. Myeloma

d. Sarcoma

c. Leukemia

Hematologic malignancy of the blood-forming elements.

a. Lymphoma

b. Sarcoma

c. Leukemia

d. Carcinoma

f. All of the above

• Viruses

• Environmental and occupational exposure

  • Ionizing and UV rad

  • Vinyl chloride, asbestos, benzene

• Lifestyle factors

• Medications

• Genetic factors

Etiology of Cancer include:

a. Viruses

b. Environmental and occupational exposure

c. Lifestyle factors

d. Medications

e. Genetic factors

f. All of the above

c. Both a and b Ionizing radiation

• Ionizing radiation

• UV radiation

• Vinyl chloride

• Asbestos

• Benzene

Environmental and occupational exposure that causes cancer includes:

a. Ionizing and UV radiation
b. Vinyl chloride, asbestos, benzene
c. Both a and b
d. Neither a nor b

• Smoking

• Diet

• Alcohol

Lifestyle factors that can cause cancer.

a. Smoking, diet, alcohol

b. Exercise, sleep, hydration

c. Vitamins, minerals, antioxidants

d. Fresh air, sunlight, rest

h. All of the above

• Change in bowel or bladder habits

• Non-healing sore

• Unusual bleeding / discharge

• Thickening or lump in breast or elsewhere

• Indigestion or difficulty of swallowing

• Obvious change in a wart or mole

• Nagging cough or hoarseness

Warning Signs of Cancer include:

a. Change in bowel or bladder habits

b. Non-healing sore

c. Unusual bleeding / discharge

d. Thickening or lump in breast or elsewhere

e. Indigestion or difficulty of swallowing

f. Obvious change in a wart or mole

g. Nagging cough or hoarseness

h. All of the above

d. Mammography

Screening test for breast cancer.

a. Fecal-Occult Blood Test (FOBT)

b. Papanicolaou Test (Pap Smear)

c. Digital Rectal Exam (DRE)

d. Mammography

c. Fecal-Occult Blood Test (FOBT)

Screening test for colorectal cancer that detects hidden blood in stool.

a. Mammography

b. Papanicolaou Test (Pap Smear)

c. Fecal-Occult Blood Test (FOBT)

d. Digital Rectal Exam (DRE)

d. Papanicolaou Test (Pap Smear)

Screening test for cervical cancer.

a. Mammography

b. Fecal-Occult Blood Test (FOBT)

c. Digital Rectal Exam (DRE)

d. Papanicolaou Test (Pap Smear)

c. Digital Rectal Exam (DRE)

Screening test for prostate and rectal cancer.

a. Mammography

b. Fecal-Occult Blood Test (FOBT)

c. Digital Rectal Exam (DRE)

d. Papanicolaou Test (Pap Smear)

b. Carcinoembryonic antigen (CEA)

Tumor marker for colorectal cancer.

a. PSA

b. Carcinoembryonic antigen (CEA)

c. Alpha-fetoprotein (AFP)

d. CA15-3

c. PSA / High acid phosphatase

Tumor marker for prostate cancer.

a. CEA

b. Alpha-fetoprotein (AFP)

c. PSA / High acid phosphatase

d. CA15-3

• ER

• PR

• CA15-3

• HER-2

Tumor markers for breast cancer include:

a. ER, PR, CA15-3, and HER-2
b. PSA and high acid phosphatase
c. CEA and AFP
d. CA19-9 and CA-125

d. Alpha-fetoprotein (AFP)

Tumor marker for liver cancer.

a. CEA

b. PSA

c. CA15-3

d. Alpha-fetoprotein (AFP)

a. CA-125

Tumor marker for ovarian cancer.

a. CA-125

b. CEA

c. PSA

d. AFP

a. Cell Cycle Non-Specific Agents

________ are not dependent on the cell being in a particular phase of the cell cycle for them to work

a. Cell Cycle Non-Specific Agents

b. Cell Cycle Specific Agents

b. Cell Cycle Specific Agents

They affect cells in all phases of the cell cycle

a. Cell Cycle Non-Specific Agents

b. Cell Cycle Specific Agents

d. G0 / Resting Phase

Phase of the cell cycle where the cell is not committed to division.

a. G1 Phase

b. S Phase

c. G2 Phase

d. G0 / Resting Phase

a. G0 Phase

Resting Phase

a. G0 Phase

b. G1 Phase

c. S Phase

d. G2 Phase

b. G1 Phase

Phase of the cell cycle where RNA and proteins are synthesized

a. G0 Phase

b. G1 Phase

c. S Phase

d. G2 Phase

b. G1 Phase

Cells grow larger.

a. G0 Phase

b. G1 Phase

c. S Phase

d. G2 Phase

c. S Phase

Phase of the cell cycle where DNA synthesis and replication occur.

a. G1 Phase

b. G2 Phase

c. S Phase

d. M Phase

c. G2 Phase

Phase of the cell cycle where DNA synthesis ceases

a. G1 Phase

b. S Phase

c. G2 Phase

d. M Phase

c. G2 Phase

Phase of the cell cycle where RNA and other enzymes (e.g., topoisomerase I and II) are produced to prepare for cell duplication.

a. G1 Phase
b. S Phase
c. G2 Phase
d. M Phase

d. M Phase / Mitosis

Phase of the cell cycle where the cell divides into two daughter cells.

a. G1 Phase

b. S Phase

c. G2 Phase

d. M Phase / Mitosis

b. Alkylating agents

MOA: Alkylation of reactive species of DNA.

a. Antimetabolites

b. Alkylating agents

c. Vinca alkaloids

d. Taxanes

g. All of the above

• Mechlorethamine

• Melphalan

• Chlorambucil

• Bendamustine

• Ifosfamide

• Cyclophosphamide

Nitrogen mustards include

a. Mechlorethamine

c. Chlorambucil

d. Bendamustine

e. Ifosfamide

f. Cyclophosphamide

g. All of the above

• Bone marrow depression

• Hemorrhagic cystitis (fibrosis of bladder)

Side effect of nitrogen mustards includes ____

a. Cardiotoxicity

b. Bone marrow depression and Hemorrhagic cystitis (fibrosis of bladder)

c. Pulmonary fibrosis

d. Ototoxicity

d. Both b and c

• Cyclophosphamide

• Ifosfamide

______ [2] are alkylating agents that causes hemorrhagic cystitis (fibrosis of bladder)

a. Melphalan

b. Cyclophosphamide

c. Ifosfamide

d. Both b and c

b. Hemorrhagic cystitis

Fibrosis of the bladder.

a. Cardiotoxicity

b. Hemorrhagic cystitis

c. Pulmonary fibrosis

d. Peripheral neuropathy

b. MESNA

Antidote for Cyclophosphamide or Ifosfamide-induced hemorrhagic cystitis.

a. Leucovorin

b. MESNA

c. Dexrazoxane

d. Amifostine

a. Amenorrhea, testicular atrophy, sterility

Nitrogen mustards affect germ cells, causing:

a. Amenorrhea, testicular atrophy, sterility

b. Cardiotoxicity, pulmonary fibrosis

c. Nephrotoxicity, ototoxicity

d. Peripheral neuropathy, hepatotoxicity

c. Nitrogen mustards

________ affect germ cells, causing amenorrhea, testicular atrophy, and sterility.

a. Antimetabolites
b. Vinca alkaloids
c. Nitrogen mustards
d. Taxanes

c. Ifosfamide

Alkylating agent that causes neurotoxicity due to its metabolite chloroacetaldehyde.

a. Cyclophosphamide

b. Melphalan

c. Ifosfamide

d. Chlorambucil

b. Chloroacetaldehyde

Ifosfamide is an alkylating agent that causes neurotoxicity due to its metabolite ________

a. Acrolein

b. Chloroacetaldehyde

c. Phosphoramide mustard

d. Carboxyphosphamide

c. Secondary malignancies

Long-term side effect of nitrogen mustards includes:

a. Hypertension

b. Diabetes mellitus

c. Secondary malignancies

d. Hyperthyroidism

c. Both a and b

• Thiotepa

• Altretamine (Hexamethylmelamine)

Ethylenimine / Methylmelamine alkylating agents include:

a. Thiotepa

b. Altretamine (Hexamethylmelamine)

c. Both a and b

b. Methylmelamines

Ethylenimine is also known as _____

a. Alkyl sulfonates
b. Methylmelamines
c. Nitrogen mustards
d. Nitrosoureas

b. Hexamethylmelamine

Altretamine is also known as _____

a. Thiotepa
b. Hexamethylmelamine
c. Busulfan
d. Cyclophosphamide

c. Busulfan

Alkyl sulfonate alkylating agent that causes pulmonary toxicity.

a. Thiotepa

b. Altretamine

c. Busulfan

d. Ifosfamide

b. Pulmonary toxicity

Busulfan is an alkyl sulfonate alkylating agent that causes ______

a. Cardiotoxicity
b. Pulmonary toxicity
c. Nephrotoxicity
d. Hemorrhagic cystitis

d. All of the above

• Carmustine

• Lomustine

• Stretozotocin

Nitrosoureas include:
a. Carmustine

b. Lomustine

c.Stretozotocin

d. All of the above

a. Nitrosoureas

Used in the treatment of brain tumors.

a. Nitrosoureas
b. Antimetabolites
c. Vinca alkaloids
d. Taxanes

c. Pulmonary toxicity

Side effect of Nitrosoureas includes:

a. Hemorrhagic cystitis

b. Cardiotoxicity

c. Pulmonary toxicity

d. Peripheral neuropathy

c. Streptozotocin

Nitrosourea used for insulinomas because it is toxic to beta cells of the islets of Langerhans.

a. Carmustine
b. Lomustine
c. Streptozotocin
d. Busulfan

b. Beta cells of islets of Langerhans

Streptozotocin is toxic to which cells of the pancreas?

a. Alpha cells of islets of Langerhans

b. Beta cells of islets of Langerhans

c. Delta cells of islets of Langerhans

d. Acinar cells

c. Both a and b

• Dacarbazine

• Temozolomide

Triazene alkylating agents include:

a. Dacarbazine

b. Temozolomide

c. Both a and b

c. Procarbazine

Methylhydrazine alkylating agent.

a. Dacarbazine

b. Temozolomide

c. Procarbazine

d. Streptozotocin

e. All of the above

• Doxorubicin

• Epirubicin

• Daunorubicin

• Idarubicin

Anthracyclines include:
a. Doxorubicin

b. Epirubicin

c. Daunorubicin

d. Idarubicin

e. All of the above

c. Mitoxantrone

Anthracenedione antibiotic.

a. Doxorubicin

b. Daunorubicin

c. Mitoxantrone

d. Idarubicin

c. Anthracyclines and Anthracenedione

MOA: Inhibits Topoisomerase II and intercalates DNA.

a. Vinca alkaloids

b. Taxanes

c. Anthracyclines and Anthracenedione

d. Antimetabolites

Side effect of Anthracyclines is _____

cardiotoxicity

c. Dexrazoxane

Antidote for side effect of anthracyclines such as “cardiotoxicity”

a. Leucovorin
b. MESNA
c. Dexrazoxane
d. Amifostine

a. Dactinomycin / Actinomycin D

MOA: Intercalates between GC base pairs of DNA.

a. Dactinomycin / Actinomycin D
b. Doxorubicin
c. Mitoxantrone
d. Plicamycin

b. GC base pairs

Dactinomycin / Actinomycin D intercalates between ______ pairs of DNA?

a. AT base pairs

b. GC base pairs

c. AG base pairs

d. CT base pairs

a. Streptomyces plicatus

Plicamycin is derived from which source?

a. Streptomyces plicatus

b. Streptomyces caespitosus

c. Streptomyces griseus

d. Streptomyces aureofaciens

b. Streptomyces caespitosus

Mitomycin is derived from which source?

a. Streptomyces plicatus

b. Streptomyces caespitosus

c. Streptomyces nodosus

d. Streptomyces venezuelae

b. L-Asparaginase

Cell cycle specific agent that acts on the G1 phase.

a. Vinca alkaloids
b. L-Asparaginase
c. Taxanes
d. Methotrexate

a. E. coli

L-Asparaginase is derived from which source?

a. E. coli

b. Streptomyces griseus

c. Penicillium notatum

d. Bacillus subtilis

b. L-Asparaginase

MOA: Hydrolyzes asparagine to aspartic acid and ammonia, thus depriving the

tumor cells of asparagine, which is needed for protein synthesis

a. Vinca alkaloids

b. L-Asparaginase

c. Taxanes

d. Methotrexate

• Topotecan

• Irinotecan

S phase specific agents that are camptothecin derivatives.

a. Topotecan and Irinotecan

b. Etoposide and Teniposide

c. Paclitaxel and Docetaxel

d. Vincristine and Vinblastine

a. Camptothecin derivatives (Topotecan, Irinotecan)

MOA: Inhibits Topoisomerase I.

a. Camptothecin derivatives (Topotecan, Irinotecan)
b. Podophyllotoxin derivatives (Etoposide, Teniposide)
c. Anthracyclines (Doxorubicin, Daunorubicin)
d. Vinca alkaloids (Vincristine, Vinblastine)

b. Cholinergic diarrhea

Irinotecan side effect is _______

a. Hemorrhagic cystitis
b. Cholinergic diarrhea
c. Pulmonary fibrosis
d. Cardiotoxicity

c. Atropine or Loperamide

Management for the side effect of Irinotecan such as “cholinergic diarrhea”

a. MESNA
b. Dexrazoxane
c. Atropine or Loperamide
d. Leucovorin

b. S phase specific agents

Topotecan and Irinotecan are classified as:

a. G1 phase specific agents

b. S phase specific agents

c. G2 phase specific agents

d. M phase specific agents

b. S phase specific agent

Hydroxyurea is classified as:

a. G1 phase specific agent

b. S phase specific agent

c. G2 phase specific agent

d. M phase specific agent

c. HydroxyureaMOA: Inhibit enzymes necessary for folic acid, DNA, or RNA synthesis.

a. Alkylating agents

b. Antimetabolites

c. Antibiotics

d. Plant alkaloids

MOA: Inhibits ribonucleotide reductase (RNR), preventing the conversion of ribo- to deoxyribonucleotides.

a. Methotrexate
b. 5-Fluorouracil
c. Hydroxyurea
d. Cytarabine

b. Antimetabolites

MOA: Inhibit enzymes necessary for folic acid, DNA, or RNA synthesis.

a. Alkylating agents

b. Antimetabolites

c. Antibiotics

d. Plant alkaloids

c. Both a and b

• Methotrexate

• Pemetrexed

Folic acid analogues include:

a. Methotrexate

b. Pemetrexed

c. Both a and b

b. Myelosuppression

Methotrexate toxicity is called _____

a. Cardiotoxicity

b. Myelosuppression

c. Pulmonary fibrosis

d. Hemorrhagic cystitis

c. Leucovorin / Folinic Acid

The antidote for methotrexate toxicity (myelosuppression) is:

a. MESNA

b. Dexrazoxane

c. Leucovorin / Folinic Acid

d. Amifostine

• Cytarabine

• 5-FU

• Capecitabine

• Gemcitabine

• 5-Azacytidine

Pyrimidine Analogues

a. 6-mercaptopurine, Fludarabine, Cladribine, Pentostatin

b. Cytarabine, 5-FU, Capecitabine, Gemcitabine, 5-Azacytidine

• 6-mercaptopurine

• Fludarabine

• Cladribine

• Pentostatin

Purine Analogues:

a. 6-mercaptopurine, Fludarabine, Cladribine, Pentostatin

b. Cytarabine, 5-FU, Capecitabine, Gemcitabine, 5-Azacytidine

c. Bleomycin

G2 phase specific agent derived from Streptomyces verticillus.

a. Etoposide

b. Teniposide

c. Bleomycin

d. Hydroxyurea

c. G2 phase specific agent

Bleomycin is classified as:

a. G1 phase specific agent

b. S phase specific agent

c. G2 phase specific agent

d. M phase specific agent

c. Bleomycin

MOA: Binds to DNA and generates free radicals.

a. Etoposide

b. Teniposide

c. Bleomycin

d. Hydroxyurea