Classification of Antineoplastic Agents

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Chapter: Medicinal Chemistry : Antineoplastic Agents

Antineoplastic agents are classified as follows: I. Alkylating agents II. Antimetabolites III. Antibiotics IV. Plant products V. Enzymes VI. Hormones VII. Immuno therapy VIII. Monoclonal antibodies IX. Radio-therapeutic agents X. Cyto-protective agents XI. Miscellaneous.


CLASSIFICATION

Antineoplastic agents are classified as follows:

I. Alkylating agents

II. Antimetabolites

III. Antibiotics

IV. Plant products

V. Enzymes

VI. Hormones

VII. Immuno therapy

VIII. Monoclonal antibodies

IX. Radio-therapeutic agents

X. Cyto-protective agents

XI. Miscellaneous.

 

I. Alkylating agents

 

a. Nitrogen mustards


Chlorambucil


Estramustine


Chloroquine nitrogen mustard

 
b. Alkyl Sulphonate

Busulfan

CH3SO2O(CH2)4OSO2CH3

 

c. Nitrosoureas


 

d. Aziridines


 

e. Altretamine


Triethylene melamine


 

f. Methylhydrazines

Procarbazine


Dacarbazine


 

II. Antimetabolites

 

a. Pyrimdine analogues


 

b. Purine Analogues


 

c. Folic acid analogues


R = H (Aminopterin)

R = CH3 (Methotrexate)


 

II. Antibiotics

 

a. Anthracyclines


Valrubicin


 

b. Bleomycins


 

c. Mitomycins

Mitomycin C


Dactinomycin C or Actinomycin D


Plicamycin or Mithramycin


 

III. Plant products

 

a. Vinca alkaloids

Vinorelbine


Vincristine, Vinblastine


Vincristine R = CHO

Vinblastine R = CH3

 

b. Camptothecin Derivatives


 

c. Epipodophyllo toxins


 

d. Taxol derivatives


 

IV. Enzymes

Examples—L-asparaginase, Pegaspargase

 

V. Hormones

 

a. Estorgenic derivatives


(i) 17-β-Estradiol R= H

(ii) Ethinyl estradiol 

Diethylstilbosterol (nonsteroidal drug)


 

b. Progestine derivatives


Progesterone


Progestins

 

c. Testosterone derivatives

Testosterone


 

d. Steroidal anti-inflammatory agents

Prednisone


Flutamide (Nonsteroidal antiandrogen)


 

d. Miscellaneous agents

Mitotane


Tamoxifen



Pipobroman


Aminoglutethimide


 

VI. Immuno therapay

Interferon α-2a; Interferon-2b; Interferon α-n3; Aldesleukin, Diftitox, Denileukin; and Bucillus calmette-Guerin (BCG)

 

VII. Monoclonal Antibodies

Rituximab, Gemtuzumab, Ozogamicin

 

VIII. Radio-therapeutic agents

Chromic phosphate P-32; Sodium phosphate P-32; Sodium iodide I-131; Strontium-89 chloride; Samarium Sm 153 lexidronam

 

IX. Cytoprotective agents

Mesna, Amifostine, Dexrazoxane

 

X. Miscellaneous



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