# A NEW CLASS OF PLATINUM ANTITUMOR DRUGS

> **NIH NIH R01** · UNIVERSITY OF VERMONT & ST AGRIC COLLEGE · 1988 · $84,704

## Abstract

DDP has become one of the most widely  used drugs in the treatment of human
tumors.  Unfortunately, the usefulness of DDP is limited by such untoward
effects as nephrotoxicity, nausea and vomiting, ototoxicity, neurotoxicity
and the potential development of resistance to DDP by the tumor cell.
During the past two years our group has synthesized in excess of 130 Pt
complexes in an attempt to develop Pt analogs possessing increased
efficacy, decreased toxicity, lack of cross resistance with DDP, or
ideally, some combination of all three attributes.  This effort has led to
the development of at least 30 compounds with significant activity.  The
purpose of the present research proposal is two-fold.  First, we intend to
continue our drug synthesis program, preparing Pt complexes altered at both
the stable amine and leaving group function alike.  We intend to
investigate the effect of diaminocyclohexane (DACH) isomers on the activity
of DACH-Pt complexes, the enhanced solubility of Pt complexes using
hydrophilic amines, the effect of mixed monodenate amines on Pt complexes
activity and, finally, the effect of leaving group substitution on water
solubility and activity of the Pt complexes.  Second, we intend to perform
chemical, biochemical and pharmacological investigations on 3 or 4 of the
most interesting Pt complexes synthesized by our group.  We have
concentrated our efforts on the development of new complexes and testing
them for efficacy and toxicity.  We now intend to study the mechanism of
action, DNA cross-linking effects, pharmacokinetics, tissue distribution,
and the sites of DNA-Pt interactions of our most exciting complexes.  In
addition, we will perform NMR, conductivity, HPLC, I.R. and, if possible,
X-crystallographic analyses of these complexes.  This approach will enable
us to better understand the chemical and biological effects of our
previously synthesized complexes while further extending our new drug
synthesis program.

## Key facts

- **NIH application ID:** 3170222
- **Project number:** 5R01CA032244-06
- **Recipient organization:** UNIVERSITY OF VERMONT & ST AGRIC COLLEGE
- **SAM.gov UEI:** Z94KLERAG5V9
- **Principal Investigator:** MILES P HACKER
- **Activity code:** R01 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 1988
- **Award amount:** $84,704
- **Award type:** 5
- **Project period:** 1982-05-01 → 1990-06-30

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/3170222

## Citation

> US National Institutes of Health, RePORTER application 3170222, A NEW CLASS OF PLATINUM ANTITUMOR DRUGS (5R01CA032244-06). Retrieved via MORVS 2026-10-25 from https://api.morvs.ai/grant/nih/3170222. Licensed CC0.

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