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Current
Bioactive Compounds
Current Bioactive Compounds
Volume 3, Number 1, March 2007
Contents
Review Articles
Editorial Pp. i
Spongiane Diterpenoids Pp. 1-36
Miguel A. González
[Abstract] [Full
text article]
Podophyllotoxin: Current Perspectives Pp.
37-66
Ying-Qian Liu, Liu Yang and Xuan Tian
[Abstract] [Full
text article]
Bioactive Compounds
Anti-Cancer/Anti-Tumor Pp. 67-74
[Full
text article]
Anti-Viral Pp. 75-78
[Full
text article]
Anti-Inflammatory Pp. 78-80
[Full
text article]
Abstracts
[Back to top]
Editorial
Structural diversity is the most important fundamental in
the modern drug discovery program. Every structural type,
in principal, is capable of locking a particular disease mechanism.
Everyday in various laboratories of the world, thousands of
structurally diverse compounds are synthesized or isolated
from natural sources. This structural diversity, if properly
harnessed, can lead to breakthrough discoveries and improve,
currently dismal, efficiency in drug development. One of the
reasons why combinatorial chemistry has not been as successful
as expected in delivering the novel molecular entities, is
inherently the low structural diversity of resulting synthetic
libraries. Medicinal chemists and other researchers involved
in drug discovery programs, therefore always look for novel
structural leads with potential to be used against specific
biological targets. The quarterly journal, “Current
Bioactive Compounds (CBC)”, thus provides an important
first set of information for drug discovery scientists. We
are glad that the journal has been very well received globally
and has already achieved a substantial subscription base in
the last two years.
Along with easy-to-read directory of newly discovered
bioactive compounds, in-depth selected reviews on
various classes of bioactive compounds have also been included
in this issue of CBC. These reviews, contributed
by leading scientists in their fields, focus on structures
and mechanisms of action of various classes most important
of bioactive chemical compounds against a range of most important
of biological disorders.
At the end, we wish to acknowledge the contributions of the
dedicated editorial and secretarial staff of the Bentham Science
Publishers. Notable among them are Mr. Mahmood Alam (Director
Publications) and his team, Dr. Ziaullah, Miss Samreen Laeeq
and Mr. Ansar Ahmed Qadri.
ATTA-UR-RAHMAN FRS
Ph.D. (Cantab.), D.Sc. (Cantab.)
M. IQBAL CHOUDHARY
Ph.D. (Kar.), D.Sc. (Kar.)
[Back to top]
Spongiane Diterpenoids
Miguel A. González
[Full
text article]
In this review we cover the structures, occurrence, biological
activities and synthesis of all the spongianes and rearranged
spongianes since their discovery in 1974. We have given special
attention to structure revisions and biological properties
of these polycyclic terpenoids of exclusive marine origin.
However, an important part of the review describes the synthetic
efforts in the field. Thus, this part has been subdivided
into syntheses from other natural products, syntheses by biomimetic
approaches and other approaches including enantioselective
total syntheses.
[Back to top]
Podophyllotoxin: Current Perspectives
Ying-Qian Liu, Liu Yang and Xuan Tian
[Full
text article]
Podophyllotoxin is a naturally occurring lignan with important
antineoplastic and antiviral properties and supported by detailed
understanding of their mechanism of action, and facilitated
by chemical manipulations that have amplified their bioactivity,
the podophyllotoxin analogues have advanced to the forefront
of several areas of therapeutic and developmental chemotherapy.
Additive and synergistic laboratory interactions with other
cytotoxic drugs have been exploited to allow development of
podophyllotoxin-based multidrug regimens, which are showing
important activity in several malignancies, and many of its
related analogues will complement conventional pharmaceuticals
in treatment, prevention and diaganosis of disease, while
at the same time adding value to agriculture. Additive and
synergistic laboratory interactions with other cytotoxic drugs
have been exploited to allow development of etoposide-based
multidrug regimens, which are showing important activity in
several malignancies. Extensive structural modifications of
podophyllotoxin have been performed in order to obtain more
potent and less toxic antitumour agents, which resulted in
the widespread clinical introduction of two semisynthetic
glucoconjugate analogues of etoposide and teniposide and newer
agents with promising preclinical activity are in various
stages of clinical assessment. As knowledge of molecular and
biochemical mechanisms of action and resistance continues
to expand, newer and better podophyllotoxin-based strategies
for treatment of malignant disease are likely to evolve. This
review provides a detailed discussion of research advances
in the synthetic and medicinal chemistry of podophyllotoxin,
and addresses the short history and pharmacological action
of these compounds and further outlines the preclinical development
and clinical trials of drugs in the pipeline and marketing
approval. Finally, a systemic evaluation of novel and important
analogues of podophyllotoxin and their contribution to the
current structure-activity profile are considered. It is hoped
that this review will be able to address the contributions
of podophyllotoxin-related research to overall drug discovery
and development and the role that this field will play in
future. |
