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

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

Abstract: The present invention provides a 3″-monohalocephalomannine of the formula: wherein R is halogen.

Abstract: 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.

Abstract: 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.

Abstract: 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.

Abstract: A device for culturing and identifying microorganisms comprising a transparent vessel with a sealable cover, a nutrient substrate carrier that can be coated with a novel growth medium and a method of using the same are disclosed. A plurality of nutrient substrates may be applied to the nutrient substrate carrier and separated into distinct zones so that a variety of microorganisms may be tested for. The method comprises innoculating the nutrient substrate with a liquid sample and incubating the nutrient substrate so that the microorganisms can be identified by visual observation of the color change of the substrate through the transparent vessel.

Abstract: 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.

Abstract: 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.

Abstract: The present invention provides for the first time an expeditious method to separate polyene macrolide antibiotics into their major components, through a general preparatory procedure employing high pressure liquid chromatography. The procedure allows for the first time a useable preparatory method for separating the polyene macrolide complexes derived from fermentation and cultivation of various organisms, into their major components. Substantially pure dermostatic A and dermostatic B can now be achieved as well as substantially pure mycoticin A and mycoticin B.

Abstract: The present invention provides a method for treating patients suffering from the acquired immunedeficiency syndrome (AIDS). The method comprises administering dermostatin, dermostatin A, dermostatin B or derivatives thereof, such as pharmaceutically acceptable esters, salts or complexes. The administration of the dermostatin or dermostatin A or dermostatin B should be done as soon as possible after the detection of the presence of the HIV virus which is believed to be responsible for the onset of AIDS. These polyene macrolide antibiotics have been found to be effective in improving the viability of lumphocyte cells infected with the HIV virus and in preventing the replication of the virus. The present invention also provides for the first time substantially pure dermostatin A and dermostatin B and an HPLC method for separation of dermostatin complex into those components in substantial purity.

Abstract: New anthracyclinones, including maggiemycin, anhydromaggiemycin and 7-oxidodaunorubicinone, have been prepared. Maggiemycin, anhydromaggiemycin, and 7-oxidodaunorubicinone all exhibit biological activity; they are toxic to cell lines KB, L1210 and P388.

Abstract: A novel plate system for thin layer chromatography comprises a supporting plate coated over about 50-90% of its area with an adsorbent layer, the uncoated surface comprising at least one strip of uniform width along an end of the supporting plate. Two such plates grafted and clamped in a lap-joint so that the edges of the adsorbent layers are in intimate contact provide an assembly on which a chromatogram developed on the first plate can be transferred in whole or in part onto the second plate. The assembly and technique are particularly useful for preparative thin layer chromatography.