# SYNTHESIS OF BIOLOGICALLY ACTIVE CYCLODEPSIPEPTIDES

> **NIH NIH R01** · UNIVERSITY OF PENNSYLVANIA · 1993 · $220,590

## Abstract

This is a resubmission of proposal 2R01 CA40081-05A1.  The principal
goal of our research program is to develop efficient, stereocontrolled
synthetic routes to biologically important cyclodepsipeptides and to
study their potential sites of activity.  We have previously
investigated the chemistry and synthesis of the didemnins.  A
significant accomplishment during this period was the revision of the
stereochemistry of the Hip unit.  We have also developed a general
synthetic strategies and methodologies that will enable us to make
modifications, either in the macrocycle or in the linear side chains.
These side chains are of utmost importance for biological activity.  Our
synthetic approach id eminently suited for modifying amino acids in the
peptide chain, and to, therefore, examine specific aspects of the
structure-activity relationships (SARs).  SARs are important, not only
for the design of improved drugs, but also for better understanding of
the mechanism of bioactivity.  Using molecular modeling programs and
chemical intuition, we have designed some analogs as reasonable entry
targets and we have devised strategies for their construction.  The
planned investigations will also contribute to the development of
biologically important cyclodepsipeptides.  The structural simplicity of
the didemnins, their potent and diverse biological activities, and their
present scarcity make synthetic investigations of these compounds an
important endeavor.

## Key facts

- **NIH application ID:** 3179574
- **Project number:** 5R01CA040081-07
- **Recipient organization:** UNIVERSITY OF PENNSYLVANIA
- **SAM.gov UEI:** GM1XX56LEP58
- **Principal Investigator:** MADELEINE M JOULLIE
- **Activity code:** R01 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 1993
- **Award amount:** $220,590
- **Award type:** 5
- **Project period:** 1985-09-30 → 1994-11-30

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/3179574

## Citation

> US National Institutes of Health, RePORTER application 3179574, SYNTHESIS OF BIOLOGICALLY ACTIVE CYCLODEPSIPEPTIDES (5R01CA040081-07). Retrieved via MORVS 2026-10-25 from https://api.morvs.ai/grant/nih/3179574. Licensed CC0.

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