The medical term for tumor (or) cancer is Neoplasm, Which means a relatively autonomous growth (or) un corodinated cell proliferation of body tissue.The branch of medicine which deals with the excessive study of neoplasm (tumor) and its development diagnosis and treatment is called “Oncology.” The term cancer was translated from a Latin word carcino i.e. Crab by celsus. For the first time Hippocrates coined the Greek word Karkinos i.e. (crab/cray fish) for malignant breast cancer Agents used to treat such abnormal cell productions are known as anti neoplastic agents.they are 1.Alkylating agents:- Nitrogen mustards Cyclophosphamide Meclorethamine 2.Antimetabolites:- purine antagonist:-6-mercaptopurine Folic acid antagonist:-methotrexate Pyrimidine antagonist:-5-flurouracil 3.Plant products:- Vinca alkaloids Vincrystine vinblastine 4.Anti biotics:- Doxorubicin Actinomycin 5.Hormonal agents: Tamoxifen Glucocorticosteroids 6.Miscellaneous:- Hydroxy urea Asparginase Public education campaigns are important in highlighting the dangers of smoking, because possibly as many as 30% of cancers are caused by smoking, excessive drinking, and hazardous solvents, as well as promoting healthy diets and lifestyles. 30% of cancers are diet related that’s why everybody should take healthy diets and lifestyles. The benefits of eating high-fibre foods, fruit, and vegetables are clear. Infact, there have been various research projects aimed at identifying the specific chemicals in these foods which are responsible for this protective property.

1. ANTI NEOPLASTIC AGENTS
1By
Nakka varshitha

2. CONTENTS
INTRODUCTION
HISTORY
EPIDEMIOLOGY
CAUSE
PATHOGENESIS
CLASSIFICATION
DIAGNOSIS
ANTI NEOPLASTICS
AGENTS
2

3. INTRODUCTION
The medical term for tumor (or) cancer is Neoplasm, Which
means a relatively autonomous growth (or) un corodinated cell
proliferation of body tissue.
CELL PRODUCTION
CELL DEGRADATION
3

4. HISTORY
 The branch of medicine which deals with the excessive study
of neoplasm (tumor) and its development diagnosis and
treatment is called “Oncology.”
 The term cancer was translated from a Latin word carcino i.e.
Crab by celsus.
 For the first time Hippocrates coined the Greek word
Karkinos i.e. (crab/cray fish) for malignant breast cancer
4

5. EPIDEMIOLOGY
FEMALE MALE
 Worldwide, it is estimated that about 20% of all deaths are cancer-
related.
 Due to varying etiologic factors, cancers of the cervix and oral cavity
are more common in India while cancers of the breast and lung are
commoner in the Western populations.
5

6. CAUSES?? 6

7. PATHOGENESIS
7

8. PATHOGENESIS
8

9. SELF SUFFICIENCY IN GROWTH SIGNALS
The mechanisms that endow cancer
cells with the ability to proliferate
can be grouped according to their
role in the growth factor–induced
signal transduction cascade and cell
cycle regulation.They are
 Growth Factors
 Growth Factor Receptors &
Non-ReceptorTyrosine Kinases
 Downstream Signal-Transducing
Proteins
 Nuclear Transcription Factors
 Cyclins and Cyclin-Dependent
Kinases
9

10. IN SENSITIVE TO ANTI GROWTH SIGNALS
 RB Gene: Governor of the Cell Cycle
 TP53 Gene: Guardian of the Genome
 Transforming Growth Factor-β Pathway
 Contact Inhibition, NF2, and APC
10

11. EVADING APOPTOSIS
• Apoptosis can be initiated through
extrinsic or intrinsic Pathways. Both
pathways result in the activation of a
proteolytic cascade of caspases that
destroys the cell.
• Mitochondrial outer membrane
permeabilization is regulated by the
balance between pro-apoptotic (e.g.,
BAX,BAK) and anti-apoptotic
molecules (BCL2, BCL-XL). BH-3–
only molecules activate apoptosis by
tilting the balance in favor of the pro-
apoptotic molecules.
11

12. SUSTAINED ANGIOGENESIS
 Vascularization of tumors is essential for their growth and is
controlled by the balance between angiogenic and
antiangiogenic factors that are produced by tumor and stromal
cells.
 Hypoxia triggers angiogenesis through the actions of HIF-1α
on the transcription of the pro-angiogenic factor
VEGF.Because of its ability to degrade HIF-1α and thereby
prevent angiogenesis, VHL acts as a tumor suppressor.
 Inheritance of germ
line mutations of VHL
causes VHL syndrome,
characterized by the
development of a variety of tumors. 12

13. LIMITLESS REPLICATIVE
POTENTIAL
 In normal cells, which lack expression of telomerase, the
shortened telomeres generated by cell division eventually
activate cell cycle checkpoints, leading to senescence and
placing a limit on the number of divisions a cell may undergo.
 In cells that have disabled checkpoints, DNA repair pathways
are inappropriately activated by shortened telomeres, leading
to massive chromosomal instability and mitotic crisis.
 Tumor cells reactivate telomerase, thus staving off mitotic
catastrophe and achieving immortality.
13

14. 14

15. TISSUE INVASION AND
METASTATIS
Ability to invade tissues, a hallmark of malignancy, occurs in
four steps:
 loosening of cell–cell contacts
 Degradation of ECM
 attachment to novel ECM components
 migration of tumor cells
15

16. CLASSIFICATION

 A disease or a growth that is
likely to get uncontrollably
worse and lead to death
MALIGNANT
TUMOR
• A growth that is not likely to
cause death
BENIGN TUMOR
16

17. 17

18. TYPES OF CANCERS
 Carcinoma
 Sarcoma
 Leukemia
 Lymphoma
 Blastoma
 Melanoma
 Adenomas
 Gliomas
 Germ cell tumors
18

19. DIAGNOSIS
 Symptomatic identification
 Lab test
 Imaging procedure
CT scan
Nuclear scan
Ultra sound
MRI
PET scan
X-rays
 Biopsy
Neddle
Endoscopy
Surgery
CT scan Ultra sound PET scan
X-rays mamograph
19

20. TREATMENT
CHEMOTHERAPHY
SURGEORY
RADIATION
20

21. Classification of anticancer agents
1.Alkylating agents:-
Nitrogen mustards
• Cyclophosphamide
• Meclorethamine
2.Antimetabolites:-
 purine antagonist:-6-mercaptopurine
 Folic acid antagonist:-methotrexate
 Pyrimidine antagonist:-5-flurouracil
3.Plant products:-
 Vinca alkaloids
 Vincrystine
 vinblastine
21

22. 4.Anti biotics:-
 Doxorubicin
 Actinomycin
5.Hormonal agents:
 Tamoxifen
 Glucocorticosteroids
6.Miscellaneous:-
 Hydroxy urea
 Asparginase
22

23. Alkylating agents
Alkylation is defined as the replacement of hydrogen on an atom
by an alkyl group.
Nitrogen mustard:-
 Nitrogenmusterds get their name because they related to sulfur
containing mustard gases used during first world war.
 These are unstable as their cytotoxic effect towards the
proliferating cell insists their use.
Structure of cyclophosphamide
Cl
Cl
N P
O
NH
O
It is 2-bis-(2-chloroethyl)amino-
perhydro-1,3,2-
oxazaphosphorinane-2-oxide mono
hydrate.
23

24. Properties
 Readily soluble in water.
 Melting point- 41-450 c.
 Soluble in alcohol, benzene, ethylene glycol,carbon- tetrachloride,
dioxane.
 It is available in tablets and injections.
Uses
 Treatment of Hodgkin's disease
 Acute lymphocytic leukemia
 Breast,cervix,lung,ovary tumors.
24

25. 25

26. Meclorethamine
• It is also known as mustine or chlormethethine.
• It is 2-chloro-N-(2-chloroethyl)-N-methylethanmine.
Cl H2C H2C
N
H2CCH2Cl
CH3
26

27. PropertiesProperties
• Mechlorethamine is available as Hcl salt.
• Mechlorethamine Hcl is white crystalline power.
• It is hygroscopic and freely soluble in water.
Uses
• Hodgkin’s disease
• Other lymphomas
27

28. Anti metabolites
• Anti metabolites are the agents which inhibit the enzymes involved in
the synthesis of DNA (or)it’s nucleotide building blocks.
• The inhibitors involved are described as antimetabolites generally the
cellular components like folic acids,purines.that are involved in the
synthesis of nucleic acids(DNA,RNA).
• Anti-metabolites inhibits nucleic acids synthesis by competitive
inhibition of cellular components.
28

29. Purine antagonist:6-mercaptopurine
• It is 1,7-dihydro-6H-purine-6-thione.
N
N
H
N
H
N
S
29

30. Properties
• It is available as yellow prisms having a decomposion
temperature of 3130c .
• It is insoluble in water, acetone, ether.
• It is soluble in alkali solutions.
Uses
 It has immunosuppressant action.
 It is used in the treatment of acute myelocytic leukemia.
30

31. Folic acid antagonist: methotrexate
• It is 4-amino-(N10)-methylpteroylglutamic acid.
O
H
N
CO2H
HO2C
N
CH3
H
N
N
H
N
NH2
NH2
31

32. Mechanism of action
32

33. properties
 Methyltrexate is available as yellow crystals having a decomposition
temperature of 2040 c.
 It is soluble in alkaline or acidic solutions .
 Insoluble in water.
Uses
 Used in the treatment of gestational choriocarcinoma.
 Trophoblstic tumors of women.
 Acute lympholytic leukemia in children.
 Psoriasis, breast, lung, cancer. 33

34. Pyrimidine antagonist
5-flurouracil:
It is chemically 5-fluro-2,4(1H,3H) pyrimidienedione.
N
H
NH
O
O
F
34

35. Properties
 white crystalline power.
 sparingly soluble in water and is a light sensitive compound.
Uses
 used in the tumors.
 used topically in treatment of basal cell carcinomas and premalignant
skin keratoses.
35

36. Vinca alkaloids
Vinblastine:
• Obtained from “cathranthus roseus”.
• Vinblastine having 2 moites.
1.Catharanthine
2.vindoline
36

37. Properties
 White to slightly yellow colour crystalline odour less powder.
 Soluble in water, methanol,ethanol,chlorform.
 Insoluble in ether having melting point 2800c.
Uses
 Testicular cancer & ovarian cancer
 Hodgkin’s disease.
 Non-Hodgkin’s lymphoma
 Kaposi’s sarcoma.
37

38. Vincrystine
• It is also obtained from the “catharanthus roseus”
38

39. properties
• white to yellow odourless crystals.
• Freely soluble in water, insoluble in ether.
• having melting point 220c.
Uses
• Acute leukemia
• Hodgkin’s lymphoma,
• Burkett's lymphoma,
• Wilm’s tumor
• Brain, lung, breast, head tumors.
39

40. Anti-biotics
• The cytotoxic nature of antibiotics used in the treatment of cancer.
Actionomycins:
• produced from “streptomyces chrysomallus”.
H
N
NH
Cl
NH3C
H3C
40

41. Properties
 Bright red rhomboid prisms, having melting point 241-2430c.
 Soluble in alcohol, propylene glycol in mixture of water & glycol.
Mechanism of action
Actinomycins interrelate into double-helical DNA and interfere with it’s
template function.
Uses
 Rabdomyosacroma&wilm’s tumor.
 Uterus & testis tumors.
41

42. Doxorubicin
Obtained from “streptomycin chrysomallus”
OCH3
OH
O
O
CCH2OH
OH
O
O
H
NH2
H
OH
H
CH3
H
H
O
H
42

43. Properties
 Orange coloured needles having melting point 204-2050c.
 Soluble in water and aqueous alcohols, methanol.
 Insoluble in acetone, benzene, chloroform, ether.
Uses
 Treatment of leukemia
 Hodgkin’s disease
 Neuroblastoma
 Breast & ovarian cancer
43

44. Hormonal agents
Adrino cortico steroids:
Prednisone :
Uses
 Adrino Cortico Carcinoma
 Prostatic Carcinoma
C
O
O
O
CH2OH
OH
44

45. Tamoxifen
H3C
OCH2CH2N(CH3)2
45
Properties
 It is fine, white odorless,
crystalline powder having
melting point of 140
 It is slightly soluble in water
and soluble in ethanol,
methanol and acetone.
Uses
Used in Advanced breast cancer.

46. Miscellaneous
Asparaginase
Uses
Used in breast cancer.
NH2
C O
CH2
CH CH3N O
O
46

47. Alternatives For Antineoplastic Agents:
 30% cancers are diet related.
 Dithiolthiones are a group of chemicals in broccoli,
cauliflower, cabbage one of which involves the activation of
enzymes in the liver to detoxify carcinogens.
 Genistein is a protective compound found in soya products.
 Antioxidant present in green tea.
47

48. CONCLUSION
 Public education campaigns are
important in highlighting the dangers
of smoking, because possibly as
many as 30% of cancers are caused
by smoking, excessive drinking, and
hazardous solvents, as well as
promoting healthy diets and
lifestyles.
 30% of cancers are diet related that’s
why everybody should take healthy
diets and lifestyles.
 The benefits of eating high-fibre
foods, fruit, and vegetables are clear.
 Infact, there have been various
research projects aimed at identifying
the specific chemicals in these foods
which are responsible for this
protective property.
48

49. 49