About: Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts

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About: Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts Goto Sponge NotDistinct Permalink

An Entity of Type : schema:ScholarlyArticle, within Data Space : wasabi.inria.fr associated with source document(s)

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts
Creator	Patil, Satish Suryanarayanan, Raj Blazar, Bruce Cuellar, Rebecca Georg, Gunda Gurvich, Vadim Lis, Lev Morgan, Monique Norris, Beverly Schumacher, Robert
Source	Medline; PMC
abstract	[Image: see text] A disodium phosphonooxymethyl prodrug of the antitumor agent triptolide was prepared from the natural product in three steps (39% yield) and displayed excellent aqueous solubility at pH 7.4 (61 mg/mL) compared to the natural product (17 μg/mL). The estimated shelf life (t(90)) for hydrolysis of the prodrug at 4 °C and pH 7.4 was found to be two years. In a mouse model of human colon adenocarcinoma (HT-29), the prodrug administered intraperitoneally was effective in reducing or eliminating xenograft tumors at dose levels as low as 0.3 mg/kg when given daily and at 0.9 mg/kg when given less frequently. When given via intraperitoneal and oral routes at daily doses of 0.6 and 0.9 mg/kg, the prodrug was also effective and well tolerated in a mouse model of human ovarian cancer (A2780).
has issue date	2015-11-24(xsd:dateTime)
bibo:doi	10.1021/acs.jmedchem.5b01329
bibo:pmid	26596892
has license	no-cc
sha1sum (hex)	dbb74d7f7208f09f5c107ecc18d9b28fcbc4d67a
schema:url	https://doi.org/10.1021/acs.jmedchem.5b01329
resource representing a document's title	Phosphonooxymethyl Prodrug of Triptolide: Synthesis, Physicochemical Characterization, and Efficacy in Human Colon Adenocarcinoma and Ovarian Cancer Xenografts
has PubMed Central identifier	PMC4678411
has PubMed identifier	26596892
schema:publication	J Med Chem
resource representing a document's body	covid:dbb74d7f7208f09f5c107ecc18d9b28fcbc4d67a#body_text
is schema:about of	named entity 'MG%' named entity 'FREQUENTLY' named entity 'INTRAPERITONEAL' named entity 'AQUEOUS SOLUBILITY' named entity 'PREPARED' named entity 'REDUCING' named entity '0.3' named entity 'GIVEN' named entity 'MODEL OF' named entity 'PHYSICOCHEMICAL CHARACTERIZATION' named entity 'XENOGRAFTS' named entity 'SYNTHESIS' named entity 'ADMINISTERED' named entity 'BCG' named entity 'DAILY' named entity 'COLON ADENOCARCINOMA' named entity 'LOW' named entity 'ANTITUMOR' named entity 'XENOGRAFT' named entity 'TRIPTOLIDE' named entity 'HUMAN' named entity 'YEARS' named entity 'EFFECTIVE' named entity 'YIELD' named entity 'EFFICACY' named entity 'OVARIAN CANCER' named entity 'HUMAN' named entity 'TRIPTOLIDE' named entity 'COLON ADENOCARCINOMA' named entity 'OVARIAN CANCER' named entity 'PH 7.4' named entity 'DOSES' named entity 'LEVELS' named entity 'MOUSE MODEL' named entity 'STEPS' named entity 'DISPLAYED' named entity 'ESTIMATED' named entity 'ORAL' named entity 'DOSE' named entity 'PRODRUG' named entity 'NATURAL PRODUCT' named entity 'PRODRUG' named entity 'EXCELLENT' named entity '0.6' named entity 'FOUND' named entity 'COMPARED' named entity 'SHELF LIFE' named entity 'A MOUSE' named entity 'ROUTES' named entity 'HYDROLYSIS' named entity 'AGENT' named entity 'TUMORS' named entity '0.9' covid:arg/dbb74d7f7208f09f5c107ecc18d9b28fcbc4d67a named entity 'prodrug' named entity 'xenograft tumors' named entity 'prodrug' named entity 'human ovarian cancer' named entity 'Triptolide' named entity 'Physicochemical' named entity 'N-iodosuccinimide' named entity 'mice' named entity 'Sigma-Aldrich' named entity 'aqueous solubility' named entity 'hydrolysis' named entity 'natural abundance' named entity 'deionized water' named entity 'monobasic' named entity 'Tris buffer' named entity 'phase I clinical trial' named entity 'ppm' named entity 'mice'

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