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

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

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

Synthesis

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.

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.

Synthesis-

STRUCTURE ACTIVITY RELATIONSHIP

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.

THANK YOU