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CONTENTS
Introduction cancer
Classification of anti cancer agents
Introduction of virus
Classification of anti viral agents
References
CANCER
Cancer or Neoplasm is a disease in which there is uncontrolled multiplication and spread within the body of abnormal forms of the bodys own cells.
Cancer harms the body when damaged cells divide uncontrollably to form lumps or masses of tissue called tumor.
Invasiveness
Metastasis
CAUSES OF CANCER
CELL CYCLE
TREATMENT OF CANCER
Chemotherapy Radiation Surgery Targeted therapy
Immunotherapy
Hormonal therapy Stem cell/ bone marrow transplantation Palliative care
Alkylating agents
Nitrogen Mustards
Eg: Mechlorethamine, Cyclophosphamide, Chlorambucil, Melphalan Ifosfamide
H
B.
Alkyl Sulfonates
Eg :Busulfan
Cl
C.
Nitrosoureas
D. Ethylenimines
Eg: Thiotepa
E. Triazenes
Eg: Dacarbazine
cyclophosphamide
II. ANTI-METABOLITES
A. Folate Antagonists
Eg: Methotrexate
B.
C.
Purine Analogues
Eg: Thioguanine (6-TG), Mercaptopurine (6-MP), Fludarabine
Pyrimidine Analogues
Eg: Cytarabine, Fluorouracil (5-FU)
O F HN
SH H N N
N H
FLUROURACIL
MERCAPTOPURINE
III. ANTI-BIOTICS
A.
1. 2. 3.
Anthracyclines
Doxorubicin Daunorubicin Idarubicin
O O OCNH2
B. C. D. E.
OCH3
Mitomycin
Epipodophyllotoxins
Eg: Etoposide,Teniposide
Taxanes
Eg: Paclitaxel
V.
ENZYMES
Eg: L-Asparaginase
C.
D. E. F.
Androgens/Anti-androgens
Eg: Flutamide
Octreotide acetate
C
N H
OH
C.
Interleukins
Eg: Aldesleukin
Hydroxyurea
Pt
H3N
Cl
cisplatin
CELL CYCLE
Antibiotics
Nitrogen mustards differs only in the nature of third groupR R may be aliphatic or aromatic An aliphatic substituent increases the speed of attacking Resonence by aromatic substituents delocalization significantly slows the intra molecular attack Nitrogen can decompose in aqueous media forms inactive de halogenated diols
MODE OF ACTION
ALKYLATING AGENTS
The agents are CCS, form reactive molecular species that alkylate nucleophilic groups on DNA bases, particularly the N-7 position of guanine. This leads to cross-linking of bases, abnormal base pairing, and DNA strand breakage.
INHIBITS
Tetrahydrofolate (FH4)
MTX(METHOTREXATE)
H2N N N
N N NH2 HN O C NH
(CH2)2
COOH
METHOTREXATE
PURINE ANALOGUES
Incorporation of the thionucleotide analogue into DNA or RNA. Feedback inhibition of purine nucleotide synthesis.
SH H N N
MERCAPTOPURINE
PYRIMIDINE ANALOGUES
- The active metabolite that inhibit DNA synthesis is the deoxyribonucleotides 5-fluoro-2-deoxyuridine 5 phosphate. - Target enzyme inhibited by 5-Fu is thymidylate synthetase.
NH2
O F HN
N H
FLUROURACIL
Uridylate (dUMP)
Thymidylate dTMP)
OHH2C
O
HO
Thymdylate synthetase
HO
CYTARABINE
ANTIBIOTICS
- It binds to DNA and inhibit the synthesis of both DNA & RNA. - Its cytotoxic action is mediated byTopo isomerase-II
O O OCNH2
OCH3
mitomycin
TUBULIN
MICROTUBULE
ENZYMES
- L-asparaginase catalyzes the hydrolysis of L-Asparagine to aspartic acid & ammonia. L-glutamic acid is also hydrolyzed by this enzyme.
HYDROLYSIS
ASPARGINE
Aspartate +
Ammonia
HORMONAL AGENTS
- Tamoxifen binds to estrogen receptors within the cell & competes with endogenous estrogen.
Estrogen
Cell death
Synthesis of cyclophosphamide
SIDE EFFECTS
Bone Marrow Suppression Gastrointestinal disorders Allopecia Phlebitis Nephrotoxicity Hepatotoxicity Cardiotoxicity Pulmonary toxicity Reproductive toxicity
ANTIVIRAL AGENTS
VIRUS
Obligate intracellular parasites Nucleic acid core: DNA or RNA Often contain virus-specific enzymes Surrounded by protein: capsid
Classification of Viruses
DNA- VIRUSES Eg: papilomavirus, Adenovirus, parvovirus, Herpes virus RNA- VIRUSES Eg: Rubella virus, Hepatitis virus, Arenavirus, Influenza virus, RITRO-VIRUSES Eg: HIV-I , HIV-2
N O
DIdanosine
O
NH
N O
H2CHO
ACYCLOVIR
O
O
NH2
NH
H2N H2CHO
N O
HO HO
OH
1-Arabinofuranosylcytosine
(cytarabine)
ACYCLOVIR
O
NH
H3C HN
O CH3 HN
N O HO
N
N
N
HO
DIdanosine
Nevirapine
Cl
Cl
N COOH
chlorambucil
Cl O
Cl O O P NH Cl N
O P N Cl NH
Cyclophosphamide
ifosfamide
O
O OCNH2
H3N
Cl
OCH3
Pt
H3N
Cl
Cisplatin
mitomycin
SH
O F HN
H N N
N
NH2
N H
FLUROURACIL
OHH2C
O
HO
MERCAPTOPURINE
HO
CYTARABINE
H2N
N N NH2 HN O C NH
(CH2)2
COOH
METHOTREXATE
These were the first type of drug available to treat HIV infection . Interfere with the action of an HIV protein called reverse transcriptase, which the virus needs to make new copies of itself.
O NH N
N O HO
DIdanosine
H3C HN N
Nevirapine