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INTRODUCTION :
In This Journal I Will Be Talk About One Of The Most Important Anticancer
Agent But First I Will Inform Some Information About Cancer Why It Is One Of
The Most Disease Affect To The Body , How Invasion The Cell Of Human Body
And Most Common Type Of Cancer In Saudi Arabia .
Also , I Wil Try To Talk About Most Important Class ( Alkylating Agent ) Why Its
Most Important And The Chemistry Of This Class .
In my journal I will try to Mention My Understand About The Topic .
Body :
Cancer is abnormal growth and division of human cell , on other mean cancer is
out of control of human cell . dangerous of cancer come from it can travel
through the body and affect to the other organ some time in very short time .
The cancer is invasive and affect the cell cycle so must be know the anti cancer
agent is based on this concept.
The most common type of cancer in Saudi even in the world the breast cancer
(20.6% by comparing other type) due to many cause no need to mention it in
this journal .
ALKYLATING AGENT : is highly electrophilic compound that react with
nucleophilic to form strong covalent bond .
electrophilic compoundrepresented by alkylating agent while nucleophilic
represented by nitrogen base of DNA .
Alkylating agent act by Alkylating DNA mainly occur in guanine base N-7 , but
also can occur in other base ( N-3 cytosine ) and (N-1 and N-3 of adnine) .
In normal cell Alkylating can be repair but still problem of Alkylating agent is
harm the normal cell .
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This structure shown site of Alkylating agent bind to any nitrogen base
nucleophilic of DNA polymer.
There is many type of Alkylating agent :
1-
Nitrogen mustard (melphalan) :
High alkylating agent activity
The chlorine , two carbon and nitrogen important for their activity .
More modification was conducted by having a moiety which mimcs the amino
acid pheylalanine , which lead to the development of melphalan .
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2- Nitrogen mustards (cyclophosphoamide) :
- most commonly used alkylating agent .
- its act as prodrug and its not toxic itself and not affect to the GIT for this reason .
- metabolized by the liver CYP450 enzymes .
-can be taken orally don’t damage GI .
- Unfortunately , the acrolein on phosohoramide responsible for kidney toxicity but it
can overcome.
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Conclusion :
Cancer is a disease of the cell so must be study the cell cycle and controlling factor also
must be design anticancer agent as key to affect to this cycle and regulation . normal cell
can be repair while cancer cell can't be repair and from this point the dangerous of
cancer come .
The growth of cancer is by growth of blood vessels (angiogenesis) so if inhibit the
enzyme responsible of angiogenesis can develop new agent of ant metastatic agent .
Alkylating agent are most important , more commonly used and first anticancer was
used so I focus about it .
The high Alkylating agent can be increase or reduced by modification of structure for
example if put aromatic ring on nitrogen atom instead of methyl group reduce activity in
case of nitrogen mustard .
There is other Alkylating agent not mention like nitrosoureas and cisplatin and
carboplatin.
Different class of anticancer is only different in mechanism of action and they have same
idea .
Alkylating agent interact directly with DNA there is another method of disturbs DNA
function by another class .