This document discusses different classes of anti-cancer agents, including targeted drugs and hormonal drugs. It focuses on imatinib, a BCR-ABL tyrosine kinase inhibitor that inhibits cancer cell proliferation and induces apoptosis. It also discusses finasteride, a 5-alpha reductase inhibitor that decreases levels of dihydrotestosterone to reduce prostate growth and hair loss by inhibiting the conversion of testosterone to DHT. The document covers the mechanisms of action, synthesis, and structure-activity relationships of these drugs. It concludes by thanking the reader and listing references used.

1. Anti- Cancer Agents
By- Siddharth Shekhar Singh
M. Pharm 1st Year

2. CLASSIFICATION
Anticancer Drugs
Targeted Drugs
BCR-ABL
tyrosine kinase
inhibitors
Imatinib
Dasatinib
Nilotinib
CD2O
Inhibitors
Rituximab
Hormonal Drugs
5 alpha
reductase
inhibitors
Finasteride
Dutasteride
Aromatase
inhibitors
Letrozole
Anastrozole

3. TARGETED DRUGS
• Imatinib-
Mechanism of action-
This inhibit BCR-ABL
tyrosine kinase inhibitor
This inhibits the
proliferation and thus,
induction of apoptosis in
cell.

4. Synthesis

5. Structure Activity Relationship
• Amide group as a substituent at phenyl group shows inhibitory action
against tyrosine kinases.
• Substitution at 6 position of diaminophenyl ring abolished the activity
against PKC.
• Introduction of methyl group in an ortho position to the amino group can
increase the selectivity of Bcr-Abl.
• Bioavailability and solubility can be enhanced by the introduction of N-
methylpiperazine group.

6. HORMONAL DRUGS
• Finasteride
Mechanism of Action-
• Competitive and specific inhibition of Type II 5α-reductase.
• This leads to the inhibition of the conversion of androgens into 5α-dihydrotestosterone (DHT).
This results in decrease in the level of DHT in the serum and increase in the level of
testosterone concentration in serum.
• DHT is the principle androgen for the prostate growth, and thus, the decrease in the level of
DHT leads in the decrease in the volume of prostate.
• Finasteride also decreases the DHT level in the scalp and thus, help in hair regrowth and slow
hair loss.

7. Synthesis-

8. STRUCTURE ACTIVITY RELATIONSHIP

9. REFRENCES
Text book of Medicinal Chemistry, volume-1, K.Ilango, P.Vlentina.
Medicinal Chemistry, second edition, D.Sriram, P.Yogeeswari.
Wilson and Gisvold’s Textbook of Organic, Medicinal and Pharmaceutical
Chemistry.

10. THANK YOU