Anti-Cancer Drugs

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Cancer is due to uncontrolled division of cells-

Cancer is neoplsam or tumor so anticancer drugs


also called as Antineoplastic agents or antitumor
agents
CANCER CHEMOTHERAPY
Chemotherapy --- 5 A
I.A- Alkylating agents-
Nitrogen Mustards-Mecholethamine,Cholrambucil,
Nitrosourea - Carmustine,Lomustine
Alkylsulfonate- Busufan
II A-Antibiotics- rubicin-(DD)- Doxorubicin, Daunorubicin,
Mycin- (ABM) - Actinomycin-D,Bleomycin, Mitomycin
III.A- Alkaloids- - Vincristine,Vinblastin
IV.A-Antimetabolites-

a)Foilc acid antagonist- Methotrexate


b)Purine antagonist- 6-MP( 6- Mercaptopurine),6-TG ( 6-
thioguanine)
c)Pyrimidine antagonist- 5-FU –(5-fluro uracil)
V A-Asparginase- Enzyme
VI - Platinum compound- Cisplatin
based on cell cycle- Due to cell cycle - cells under go uncontrolled division
causes cancer .So anti cancer drugs inhibits cell cycle.
Cell cycle is divided in to 4 phases---- G1, S, G2, ( called as
Interphase),
M – Mitotic phase
I. Cell cycle specific Drugs (CCS) ---Drugs selectively inhibits particular
phase of cell cycle
G1 Phase blocking agents- Enzymes- Asperginase
S-phase blocking agents- Ant metabolites -Methotrexate,6-MP,6-TG, 5-FU
G2 –phase blocking agents- Antibiotics Bleomycin
M- phase blocking agents– Anti mitotic drugs- - Vinca alkaloids
II Cell cycle Non specific drugs( CCNS )- these drugs can block any
phase of the cell cycle
(ACD)
Example- A -Alkylating agents
C- Cisplatin
D-Doxorubcin
Anti Metabolites
Antimetabolites inhibits S phase of cell cycle
Drugs Inhibits synthesis of DNA the following way
a) By Inhibiting Foilc acid synthesis
( folic acid antagonist- Methotrexate,)
b) By Inhibiting Purine synthesis
Purine antagonist - 6-MP( 6- Mercaptopurine),
6-TG ( 6-thioguanine)
c) by Inhibiting Pyrimidine synthesis
Pyrimidine antagonist - 5-FU –(5-fluro uracil)
a) Antifolate- Methotrexate
Folic acid antagonist – Methotrexate – It inhibits Dihydo folate reductase
enzyme .there by reduce synthesis of Tetrahydrofolic acid .It leads reduce
synthesis of DNA in the cells .
S
D

P
Methotrexate
P

9
5 FU-flurouracil – pyrimidine antagonist (inhibits nucleic acid
synthesis)
5- FU when enters to cancer cell converted into 5-Fdump
which inhibits thymidylate synthease enzyme there by reduce
synthesis of DNA and 5 FUTP which inhibits RNA synthesis
5 FU
( protein synthesis)

5-dUMP 5-F UTP

Inhibits thymidylate
synthease

Inhibits RNA
Inhibits DNA synthesis synthesis
DNA- Alkylating agents
These act as Cell cycle non specific drugs
These agents transfer alkyl group to DNA and form Irreversible
covalent bond with DNA ( at between Guanine residues)

It leads to
 Damage of DNA-
Miscoding of DNA bases
Prevent DNA Replication
Example
Nitogen mustards
Carmustine
Busulfan
Antibiotics

Anthracyclines Non-anthrcyclines
Ex- Ex Mycins(MBA)
Rubicins-DD Mitomycin Bleomycin
Daunorubicin Actinomycin-D ( Dactinomycin)
Doxorubicin
Actinomycin-D act as peptide derivative act as DNA Intercalating agent

Bleomycin - It is a glycopeptide antibiotic,


generates free radical and Damages DNA
It inhibits G2 Phase of Cell cycle
Mitomycin acts as DNA alkylating agent
Doxorubicin acts As Topoisomerase-II enzyme
blocker
Alkaloids
Vinca alkaloids - Vincristine and Vinblastine -
Obtained from leaves of plant catharanthus
roseues.

These drugs block M - phase of cell cycle

Inhibits mitotic of cells so called as antiMiotic


drugs

catharanthus roseues.

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