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Abstract

Abstract: The objective of the proposed research is to synthesize acyl, carbamyl and carbonate derivatives of demethypenclomedine (DM-PEN), the antitumor active, non-neurotoxic metabolite of penclomedine (PEN), a clinically- evaluated drug whose development was terminated because of clinical neurotoxicity. The three series of novel agents will be evaluated in a human breast tumor xenograft (MX-1) and in a human CNS tumor xenograft (U251) implanted subcutaneously (sc) or intracerebrally (ic), respectively, to provide data for selection of a clinical candidate for proposed further development in Phase II of this fast track application. PEN, DM-PEN and the acetyl derivative of DM-PEN were all active against ic-implanted MX-1 tumor, and PEN and DM-PEN were active against a series of human brain tumor xenografts (gliomas, ependymonas) implanted sc. The primary goal of this project is to evaluate derivatives of DM-PEN in the clinical treatment of brain tumors since the former and its acetyl derivative have been shown to be active against ic-implanted MX-1 tumor, and PEN and DM-PEN were active against a series of human gliomas and ependymomas implanted sc. PROPOSED COMMERCIAL APPLICATIONS: The potential commercial application of this research is the synthesis of a novel derivative of DM-PEN that may be of clinical benefit for the treatment of brain tumors or other types of cancer.

Thesaurus Terms:
analog, antineoplastic, chemical structure, drug design /synthesis /production, pyridine
brain neoplasm, breast neoplasm, drug screening /evaluation
chemical synthesis, laboratory mouse, mass spectrometry, nuclear magnetic resonance spectroscopy, thin layer chromatography

Institution:	DEKK-TEC, INC.
	4200 CANAL ST, STE A
	NEW ORLEANS, LA 70119
Fiscal Year:	2002
Department:
Project Start:	01-MAY-2000
Project End:	30-APR-2004
ICD:	NATIONAL CANCER INSTITUTE
IRG:	ZRG1