This document discusses anticancer drugs and their mechanisms of action. It begins by defining cancer and describing different types. Anticancer drugs are then classified into groups including alkylating agents, antimetabolites, antibiotics, plant products, and hormones. The mechanisms of several drug classes are explained, such as how alkylating agents form reactive groups that bind to and break DNA. Newer drugs like temozolomide and pemetrexed are also introduced along with their uses and mechanisms. In summary, the document provides an overview of cancer types and classifications, along with explanations of established and newer anticancer drug mechanisms of action.

1. ANTICANCER DRUGS
Presented by: Tanusree Manna
M.Pharm (Pharmaceutical Chemistry)
1ST Year, 1ST Sem
Bharat Technology

2. Contents
• Introduction
• Classification of different types of cancers
• Classification of anticancer drugs
• Mechanism of action of various anticancer drugs
• Newer drugs
• Reference
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3. Introduction
• Cancer is a disease characterized by an abnormal and
uncontrolled division of cells in a part of the body and then
spread to other parts of the body.
• A malignant growth or tumour resulting from an uncontrolled
division of cells.
• Cancer cells separate themselves from primary tumour and are
carried by the lymphatic system, reaches distant sites of organs
where they divide and form secondary tumours.
• Cancer is caused by- smoking, exposure to toxic chemicals and
radiant energy.
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4. Classification of different types of cancers
• Carcinoma- This type of cancers affects organs and glands,
such as the lungs, breasts, pancreas, prostate etc.
• Sarcoma- This type of cancer affects soft or connective tissues,
such as muscle, cartilage etc.
• Melanoma- This is a type of skin cancer.
• Lymphoma- A cancer of the lymphatic system.
• Leukemia- This is a type of blood cancer. Leukemia is cancer of
blood-forming tissues, including bone marrow.
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5. Classification of anticancer drugs
Anticancer or antineoplastic agents are used for the treatment of cancer. Classification of
anticancer drugs are given below-
1. Alkylating agents:-
i. Nitrogen mustard: Mechlorethamine, chlorambucil, cyclophosphamide, estramustine.
ii. Nitrosourea: Carmustine, lomustine.
iii. Aziridines: Thiotepa, benzotepa.
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6. iv. Aryl sulphonates: Busulphan.
v. Miscellaneous: Dacarbazine.
2. Antimetabolites:
i. Folic acid antagonist: Methotrexate.
ii. Purine antagonist: 6-mercaptopurine, 6-thioguanine.
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7. iii. Pyrimidine antagonist: 5-fluoro uracil.
3. Antibiotics: Daunorubicin, doxorubicin.
4. Plant products: Vinca alkaloids- Vincristine, vinblastine.
Taxol derivatives: Paclitaxel, Docitaxel.
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8. Podophyllotoxin: Etoposide, Teniposide.
5. Hormones: Tamoxifen, flutamide.
6. Miscellaneous: Procarbazine, cisplatin.
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9. MECHANISM OF ACTION OF VARIOUS ANTICANCER
DRUGS
• MOA of Alkylating agents:
Alkylating agents
Forms highly reactive carbonium ion
Transfers alkyl groups to N-7th position of guanine of DNA
Results in
Abnormal base pairing DNA strand breakage
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11. • MOA of Antimetabolites:
Folic acid antagonist
Inhibits enzyme dihydrofolate reductase(DHFR)
Production of purine and pyrimidine gets hampered
Purine antagonist
Inhibit the production of purine containing nucleotides(Adenine and guanine)
Pyrimidine antagonist
Inhibits the production of Pyrimidine containing nucleotides(Cytosine and
thymine for DNA, Uracil and Cytosine for RNA)
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13. • MOA of Natural products:
Vinca alkaloids (Vincristine and vinblastine)
Arrest cell division in metaphase
Binds to tubulin and prevents its polymerization into microtubules
Taxol derivatives (Paclitaxel and Docitaxel)
Stabilizes and prevents microtubule depolymerization
Leading to cell cycle arrest and cell death
Podophyllotoxin (Etoposide and Teniposide)
It prevents topoisomerase II (Topo II)
Prevents unfolding of DNA
Prevents DNA synthesis
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14. 1
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15. • MOA of Antibiotics:
Antibiotics
Binds to DNA Inhibits mitosis
Inhibits nucleic acid synthesis Prevents cell division
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16. Newer drugs
1. Temozolomide:
• It is an imidazotetrazine derivative of the alkylating agent
dacarbazine.
• It is a prodrug and undergoes rapid chemical conversion in the
systemic circulation at physiological pH.
• It is used for the treatment of cancerous brain tumor.
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17. 2. Pemetrexed:
• It is chemically similar to folic acid.
• It is approved for the treatment of lung cancer (a type of
tumour in the lining of the lung) in combination with cisplatin.
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18. Reference
• Medicinal Chemistry, 2nd edition, D. Sriram, P. Yogeeswari.
• Wilson and Gisvold’s Textbook of Organic, Medicinal and
Pharmaceutical Chemistry, 12th edition, John M. Beale Jr., John
H. Block.
• Textbook of Medicinal Chemistry, 3rd edition, Volume 2, V.
Alagarsamy.
• Google images.
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19. THANK YOU…