Xechem International, Inc.

Luben K. Yankov

Ramesh C. Pandey

Alex Poulev

Raghu Nair

Luben K Yankov

Ramesh C Pandey

Alex Pouley

This invention is directed to novel halogenated paclitaxel derivatives, processes for their preparation and use as effective anti-tumor agents.

Halogenated paclitaxel derivatives

The present invention provides a 3&Prime;-monohalocephalomannine of the formula:

Monohalocephalomannines having anticancer and antileukemic activity and method of preparation therefor

Provided are novel paclitaxel analogues which are selectively chlorinated stereospecific derivatives of cephalomannine and 7-epi-cephalomannine having paclitaxel-like antitumor efficacy, methods for their preparation and methods for treating tumors with these compounds.

Preparation of chlorinated paclitaxel analogues and use thereof as

Provided are antineoplastic derivatives by a process of selective halogenation of side chains of unsaturated taxanes; more particularly, the process involves the use of halogens, particularly bromine, which is easily added to the side chain double bond of cephalomannine, leaving paclitaxel unchanged, and wherein diastereomeric mixtures of 2', 3'-dibromocephalomannine display high activity against: Leukemia cell line HL-60 (TB); Non-Small Cell Lung Cancer line NCI-H522; Colon Cancer cell lines COLO 205 and HT 29; CNS Cancer cell lines SF-539 and SNB-75; Ovarian Cancer Cell line OVCAR-3; Renal Cancer cell line RXF-393; and Breast Cancer cell lines MCF7, MDA-MB-231/ATCC, HS 578T, MDA-MB-435 and MDA-N.

Dihalocephalomannine and methods of use therefor

Method for production of 2', 3' dihalocephalomannine

Provided are novel paclitaxel analogues, namely selectively brominated stereospecific derivatives of cephalomannine and 7-epi-cephalomannine having in vivo and in vitro paclitaxel-like antitumor efficacy, methods of preparation therefor and methods for treating tumors with these compounds.

Preparation of brominated paclitaxel analogues and their use as

A novel process for extraction, isolation and separation of taxanes, particularly paclitaxel, from natural sources such as bark, needles and twigs from Taxus species, tissue cultures, and fungi is described, wherein the taxanes are separated from the crude extracts by partitioning between polar and nonpolar solvents, precipitation in nonpolar solutions, reacting the mixture by halogenation of unsaturated taxane derivatives, followed by chromatographically separating and crystallizing taxanes from a mixture of polar and nonpolar solvents; more particularly, the process of halogenation of unsaturated side chain taxane derivatives, particularly cephalomannine in presence of paclitaxel, is described, wherein bromine is preferably added to the double bond of unsaturated taxanes leaving paclitaxel unchanged, with paclitaxel being easily separated from the mixture including the less polar halogenated taxane derivatives.

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Edison, NJ, United States of America

Luben K Yankov