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Lignans as Anticancer Agents (Paperback)
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Lignans as Anticancer Agents (Paperback)
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Cancer, an abnormal and uncontrolled cell division, has engulfed
the lives of unlimited people till date. Etoposide and Teniposide
are podophyllotoxin derivatives and have been used clinically for
treatment of refractory testicular tumor and cancer. These
compounds arrests cell growth by DNA topo II inhibition, which
causes double strand breaks in DNA and known as non-interclating
topo II inhibitors. They have many side effects, such as
myelosuppression, poor water solubility, and the development of
resistance so modification is done on it at various sites.
Podophyllotoxin contains a five-ring system. Modification of the
A-ring gave compounds having significant activity but less than
that of Etoposide, whereas modification of the B-ring resulted in
the loss of activity. E-ring is essential for its anticancer
activity and D-ring in lactone form is preferred for better
activity. The introduction of double bond in C-ring lowers the
activity but modifications at the C-4 in C-ring with bulkier groups
enhance anticancer activity. NK-611, GL-331 and Etoposide phosphate
are water soluble derivatives of Etoposide with potent anticancer
activity and are currently in clinical trials.
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