IUPAC nomenclature

(SP-4-2)-diamminedichloroplatinum(II)

Classification

Cisplatin  falls under the category of Antineoplastic cytotoxic drug. [1]

Physiochemical Properties

Mechanism of Action                                                                                                                       

i. It introduces the alkyl groups to the DNA. When repair enzymes tries to remove the alkylaed fragments, they fragment the DNA.

ii. It binds with DNA and produces cross-linkages.

iii. It induces mispairing of the DNA causes mutations in the cells.[2]

Structural Activity Relationship

• Cytotoxicity of oxiplatin is also greater than cisplatin.
• Organic functionalities of nonleaving groups coordinated to platinum are critical for selective uptake by OTCs. [3]

Methods of Synthesis

i. Potassium tetrachloroplatinate is reacted with excess of potassium iodide.

ii. The tetraiodide so formed is reacted with ammonia to form K₂[PtI₂(NH₃)₂], a yellow compound.

iii. The insoluble silver iodide is precipitated as the yellow compound is treated with silver nitrate in water.

iv. Addition of the potassium chloride gives the final product.

Therapeutic Uses

Cisplatin is given for the treatment for :

• Mesothelioma
• Melanoma
• Multiple myeloma
• Sarcomas
• Neuroblastoma
• Hodgkin’s lymphomas
• Non-Hodgkin’s lymphoma
• Prostate cancer
• Stomach cancer
• Cerviacal cancer
• Breast cancer
• Small cell lung cancer
• Non-small cell lung cancer
• Esophageal cancer
• Head and neck cancer
• Bladder cancer
• Ovarian cancer
• Testicular cancer
• Metastatic cancer
• Metastatic ovarian cancer
• Advanced bladder cancer

Side Effects

• Common side effects of cisplatin include nausea, vomiting, low blood counts, kidney toxicity, ototxicity and blood test abnormalities.
• Less common side effects of cispatin include peripheral neuropathy, loss of appetite, taste changes, increase in blood tests measuring liver function and hair loss.

MCQs

Q.1 Match the following with correct IUPAC nomenclatures

a) i-A, ii-C, iii-B

b) i-B, ii-A, iii-C

c) i-C, ii-B, iii-A

d) i-C, ii-A, iii-B

Q.2 How many statements below are true with respect to the SAR of the drug cisplatin?

• Trans form is less cytotoxic than cis form.
• Cytotoxicity of oxiplatin is greater than cisplatin.
• Organic functionalities of nonleaving groups coordinated to platinum are critical for selective uptake by OTCs.

a) 1

b) 2

c) 3

d) 0

Q.3 The drug cisplatin is found in which form

a) Lyphophillized powder form

b) Hydrophillized powder form

c) Can be in either of lypopyhllized or hydrophyllized powder form

d) None of the above

Q.4 The number of incorrect statements with respect to the method of synthesis of the drug cisplatin is?

• Synthesis starts with potassiumtetrachloroplatinate.
• K₂[PtI₂(NH₃)₂ is a red colored compound.
• The final product is obtained after addition of potassium cyanide

a) 1

b) 2

c) 3

d) 0

Q.5 Which amongst the following is not a therapeutic use of drug cisplatin?

a) Down’s diseases

b) Hodgkin’s lymphomas

c) Non-Hodgkin’s lymphomas

d) Small-cell lung cancer

Q.6 The correct classification of the drug cisplatin can be?

a) Calcium channel blocker

b) Antiarrhythemic drug

c) Antineoplastic cytotoxicity drug

d) Immuosuppressive agent

Q.7 How many number of rings are found in the chemical structure of the drug cisplatin?

a) 0

b) 1

c) 2

d) 3

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ANSWERS

1-d

2-b

3-a

4-a

5-a

6-c

7-a

REFERENCES

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IUPAC nomenclature

Cis diammine(cyclobutane-1,1-dicarboxylate-O,O’)platinum(II)

Classification

Carboplatin falls under the category of Antineoplastic cytotoxic drug. [1]

Physiochemical Properties

Mechanism of Action

i. It introduces the alkyl groups to the DNA. When repair enzymes tries to remove the alkylated fragments, they fragment the DNA.

iii. It binds with DNA and produces cross-linkages.

iii. It induces mispairing of the DNA causes mutations in the cells.[2]

Structural Activity Relationship

• A leaving group is necessary for the activity.
• Cytotoxicity of oxiplatin is also greater than carboplatin.
• Organic functionalities of nonleaving groups coordinated to platinum are critical for selective uptake by OTCs

Methods of Synthesis

i. Cisplatin is reacted with silver nitrate to form cis-diamino-(1,1-cyclobutandicarboxylate)platinium(II).

ii. The above formed compound is then reacted with cyclobutan-1,1-dicarboxylic acid to form carboplatin.

Therapeutic Uses

Carboplatin is used for the treatment of:

• Ovarian cancer
• Osteogenic sarcoma
• Germ cell tumors
• CNS tumors
• Cervical cancer
• Breast cancer
• Bladder cancer
• Esophageal cancer
• Endometrial cancer
• Head and neck cancer
• Lung cancer

Carboplatin is also used for the preparation of the germ cells and during the bone marrow transplant.

Side Effects

• The common side effects of carbolatin include low blood counts, nausea, vomiting, tatste changes, loss of hair, weakness and blood test abnormalities.
• Some of the less common side effects of carboplatin are abdominal pain, diarrhea, burning sensation at injection site, constipation, mouth sores, peripheral neuropathy, central neurotoxicity, nephrotoxicity, ototoxicity, abnormal blood electrolyte levels, abnormal blood liver enzymes, some cardiovascular abnormalities and allergic reactions.

MCQs

Q.1 Which term is associated with the drug carboplatin?

a) Kemocarb

b) Oncocarbin

c) Shantinib

d) Both a) and b)

Q.2 Match the following with respect to the physical forms of drugs

 a) i-C, ii-A, iii-D, iv-B

b) i-A, ii-D, iii-B, iv-C

c) i-C, ii-B, iii-A, iv-D

d) i-B, ii-A, iii-C, iv-D

Q.3 The drug Carboplatin shows its action through?

a) Introduction of tyrosyl group

b) Alkylation of DNA

c) Interacting with cellular enzymes

d) None of the above

Q.4 The correct order for the synthesis of the drug carboplatin is?

I. Reaction of cisplatin with silver nitrate

II. Reaction of cisplatin with Potassium dichromate.

III. Reaction with cyclobutan-1,1-dicarboxylic acid.

IV. Reaction with cyclopropane-1,1-dicarboxylic acid.

a) I – III

b) I – IV

c) II – III

d) II – IV

Q.5 Predict the incorrect statements from the following with respect to the classification of the drug.

I. Vincristine is an epipodophyllotoxin

II. Cytarabine is a pyrimidine antagonist.

III. Carboplatin is an antineoplastic drug.

IV. Flutamide is an antiandrogen.

a) I, II & III

b) I only

c) III and IV

d) None

Q.6 The correct sequence of True and False for the given statements with repects to the side effects of drug Carboplatin is?

I. Low blood count is a common side effect.

II. Blood tests abnormalities may occur.

III. Central neurotoxicity is a less common side effect.

IV. Hearing loss may occur

a) TTTT

b) FFFF

c) TFTF

d) TTFT

Q.7 Which amongst the following drugs is having highest number of ring system in its structure-

a) Cisplatin

b) Dacarbazine

c) Methotrexate

d) Carboplatin

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ANSWERS

1-d

2-a

3-b

4-a

5-b

6-a

7-c

REFERENCES

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IUPAC nomenclature

{11-Amino-7-methoxy-12-methyl-10,13-dioxo-2,5-diazatetracyclo[7.4.0.02,7.04,6]trideca-1(9),11-dien-8-yl}methyl carbamate.

Classification

Mitomycin C falls under the category of antibiotic Antineoplastic cytotoxic drug. [1]

Physiochemical Properties

Mechanism of Action

i. Mitomycin gets activated to bifunctional and trifunctional alkylating agent

ii. It binds with DNA and produces cross-linkings.

iii. DNA synthesis and DNA functions are inhibited and disturbed.[2]

Structural Activity Relationship

• Electron donating substituent increases the anticancer activities.
• The attached groups on N-1 positions are responsible for different biological activities of drug.
• Methylene bridge between the anthraquinone scaffold and aromatic ring can be neglected.
• When methylene groups are removed, substitution at ortho and para positions will increase the activity of drug.
• Counter ions of the anthraquinone are not responsible for anticancer activity.
• Strong electron donating groups can significantly increase the anticancer activity of drug. [3]

Methods of Synthesis

i. Compound (A) is treated with ammonia in methanol at room temperature to get the intermediate compound (B).

ii. (B) undergoes Michael addition to give an unstable compound (C).

iii. After Beta-elimination of the compound (C), Mitomycin C can be obtained.

Therapeutic Uses

Mitomycin is used for the treatment of:

• Adenocarcinoma
• Anal cancer
• Bladder cancer
• Breast cancer
• Cervical cancer
• Colorectal cancer
• Head and neck cancer
• Non-small cell lung cancer

Side Effects

• Common side effects include fatigue, low blood counts, poor appetite and mouth sores.
• Some people may suffer from side effects like bladder inflammation, loss of hair, diarrhea, nausea and vomiting.

MCQs

Q.1  Which amongst the following is the trade name of drug Mitomycin C?

a) Mutamycin

b) Novantrone

c) Blenoxane

d) None of these

Q.2 Predict the incorrect statement related to the therapeutic uses of drug Mitomycin C.

a) It is used for treatment of anal and bladder cancer.

b) It is not used for the treatment of pneumonia

c) It is used for the treatment of head and neck cancers

d) It is not used for the treatment of colorectal cancer

Q.3 Match the following with respect to the SAR of drug Mitomycin-

 a) i-C, ii-D, iii-B, iv-A

b) i-A, ii-C, iii-D, iv-B

c) i-B, ii-D, iii-A, iv-C

d) i-A, ii-D, iii-B, iv-C

Q.4 Which amongst the following drugs shows its effect through introduction of cross-linkages between the DNA strands?

a) Letrozole

b) Mitomycin C

c) Vincristine

d) Nafarelin

Q.5  Mitomycin C drug belongs to which class?

a) Antibiotic antineoplastic drug

b) Aromatase inhibitors

c) Alkylating agent

d) Both a) and c)

Q.6 Which of the following is not a side effect of Mitomycin C?

a) low blood counts

b) Poor appetite

c) Hair loss

d) None of the above

 Q.7 Which amongst the following drugs is having least number of ring system in its structure-

a) Mitomycin C

b) Daunorubicin

c) Mitoxantrone

d) Bleomycin

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ANSWERS

1-d

2-d

3-a

4-b

5-d

6-d

7-c

REFERENCES

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