Ru*L,.,
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FOR IMMEDIATE
#L20292-02
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For Information:
Sue Pondrom
(6r-9) 554-8290 office
(5L9) 45O-O520 home
RELEASE
I{EDIA
ADVISORY
i'OLI,A RESEARCHERS ARE FIRST TO ACHIEVE TOTAIJ SYNTHESTS
OF NATURAL FORIIT OF COII(PLEX CALICHEAITTICIN UOLECUIJE
fnplications
WHAT:
for
Future
Anti-Cancer
Agent
A team of researchers
led by K.C. Nicolaou,
Ph.D. has
reported
in this week's issue of the Journal of the
(JACS) the first
American Chemical Society
total
synthesis
of calichearnicin
in its naturally
occurring
form.
The work is a major accornplishment;
for years, the
nation's
top synthetic
organic chemists have attempted
to synthesize
this remarkably cornplex molecular
structure.
WHO:
Dr. Nicolaou is the Darlene Shiley Professor and
chairman of the Department of Chemistry
at The Scripps
Research fnstitute;
and a professor
of chemistry
in the
Department of Chemistry,
University
of California,
San
Diego. Both institutions
are located in La Jo1la,
California.
Additional
authors of the journal
article
were UCSD
graduate students C.W. Hummel and E.N. Puitsinos;
and
M. Nakada, A.L. Smith, K. Shibayama, and H. Saimoto,
all postdocs at TSRI.
BACKGROUND: Calicheamicin
is a member of the enediyne class of
anti-cancer
antibiotics
which are produced by bacteria
found in soil.
Additional
enediynes are dynemicin,
the
esperamicins,
and neocarzinostatin
chromophore.
Although enediynes have been studied since 7987 for
their
ability
to cleave DNA and kill
cancer ce1ls,
the
naturally-occurring
antibiotics
are toxic
to healthy
cells as weI1.
Page 2
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of the enediyne "i;:l;":5
dynemicin,
which appeared to be
potent antiable to take advantage of an enediyners
cancer activity,
while leaving healthy
cells
intact.
The molecule they synthesized
was a simpler version
the true,
naturally-occurring
dynenicin
enediyne.
of
with the total
synthesis
of calicheamicin,
Nicolaou
rrwe can now use the same methodology
notes that
to make
variations
that may be simpler,
even better
than the
naturally
occurring
substances. rl
FOR COMMENTON THE SYNTHESIS OF CALICHEAMICIN:
K.C. Nicolaou
(61e) s54-34s8
George Ellestad,
(e14) 732-42e4
Lederele
Stuart L. Schreiber,
( 6 1 , 7) 4 9 5 - 5 3 t _ 8
Laboratories
Harvard
University