123065-60-1Relevant academic research and scientific papers
Study on the structure-activity relationship of dihydroartemisinin derivatives: Discovery, synthesis, and biological evaluation of dihydroartemisinin-bile acid conjugates as potential anticancer agents
Bian, Hongzhu,Dong, Xun,Fu, Rong,Li, Congcong,Liu, Chang,Shen, Zhengwu,Xu, Wei,Xu, Zhenye,Zhang, Jinghua,Zhao, Xiaozhen,Zou, Xiaosu
, (2021)
A series of dihydroartemisinin derivatives was synthesized, and their anti-proliferation activity against cancer cells was evaluated. Structure-activity relationship studies led to the discovery of dihydroartemisinin-bile acid conjugates that exhibit broa
A comparison of X-ray crystal structures including methyl 3,5-bis(hydroxymethyl)benzoate, its phenylethynyl extended derivative in polymorphous forms and the corresponding carboxylic acids
Katzsch, Felix,Eissmann, Diana,Weber, Edwin
experimental part, p. 245 - 255 (2012/08/28)
Considering the specific supramolecular synthon design of carboxylic acid and alcoholic hydroxyl groups in the field of crystal engineering, we compared the solid state structures of particular benzoates and corresponding acids 1-4 both in the non-spacered (1, 2) and spacered (3, 4) forms. Based on the single crystal X-ray study, there is only a slight influence of the phenylacetylene spacer with regard to the layer lattice arrangement of the benzoates while referring to the benzoic acid analogues the addition of the spacer gives rise to a modification of the lattice from a layer to a tape structure. Dependent on the crystallization conditions, two crystalline polymorphs of compound 3 (3a, 3b) were obtained and discussed regarding their structural differences. Springer Science+Business Media, LLC 2011.
New water-soluble polyanionic dendrimers - Phosphoric and 1,3,5-benzenetricarboxylic acid derivatives
Salamonczyk, Grzegorz M.
, p. 10209 - 10217,9 (2020/09/02)
Simple, very efficient, and having some aspects of generality, synthesis of water-soluble, polyanionic dendrimeric polyesters with different size, polarity, and flexibility is described. These macromolecular compounds consisting of phosphate or thiophosph
Nitric oxide enhancing diuretic compounds, compositions and methods of use
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Page/Page column 63, (2008/06/13)
The invention describes novel compositions and kits comprising at least one nitric oxide enhancing diuretic compound, or pharmaceutically acceptable salts thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating conditions resulting from excessive water and/or electrolyte retention; (b) treating cardiovascular diseases; (c) treating renovascular diseases; (d) treating diabetes; (e) treating diseases resulting from oxidative stress; (f) treating endothelial dysfunctions; (g) treating diseases caused by endothelial dysfunctions; (h) treating cirrhosis; (j) treating pre-eclampsia; (k) treating osteoporosis; (l) treating nephropathy; (m) treating peripheral vascular diseases; (n) treating portal hypertension; (o) treating central nervous system disorders; (p) treating metabolic syndrome; (q) treating sexual dysfunctions; and (r) hyperlipidemia. The nitric oxide enhancing diuretic compounds comprise at least one nitric oxide enhancing group linked to the diuretic compound through one or more sites such as carbon, oxygen and/or nitrogen via a bond or moiety that cannot be hydrolyzed.
TRICYCLIC DERIVATIVES OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, THEIR PREPARATIONS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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Page 70, (2010/02/10)
The present invention relates to tricyclic derivatives or pharmaceutically acceptable salts thereof, their preparations and pharmaceutical compositions containing them. More precisely, the present invention relates to tricyclic derivatives as colchicine derivatives, pharmaceutically acceptable salts thereof, their preparations and pharmaceutical compositions containing them. Tricyclic derivatives of the present invention show very powerful cytotoxicity to cancer cell lines but were much less toxic than colchicine or taxol, confirmed through animal toxicity test. Tricyclic derivatives of the invention also decrease the volume and weight of a tumor and have a strong angiogenesis inhibiting activity in HUVEC cells. Thus, tricyclic derivatives of the present invention can effectively be used as an anticancer agent, anti-proliferation agent and an angiogenesis inhibitor.
Synthesis of 3,5-bis(phosphonomethyl)benzoic acid and its application as a metal oxide surface bivalent anchor
Nakhle, Bassam M.,Trammell, Scott A.,Sigel, Keith M.,Meyer, Thomas J.,Erickson, Bruce W.
, p. 2835 - 2846 (2007/10/03)
A protected form of 3,5-bis(phosphonomethyl)benzoic acid (Bpb-OH), a metal oxide surface bivalent anchor, has been synthesized, coupled to an amine functionality, deprotected, and shown to bind to metal oxide surfaces. The protected anchor, 3,5-bis(dimethoxyphosphinylmethyl)benzoic acid (Me4Bpb-OH) was synthesized in 23% yield over four steps, coupled to a proline-chromophore, deprotected with a solution of iodotrimethylsilane (TMSI) in acetonitrile and adsorbed to Tin(IV)-doped indium oxide and nanocrystalline TiO2 electrodes at surface coverages of 1.5 x 10-10 mol cm-2 and 4.9 x 10-11 mol cm-2, respectively. Finally, Me4Bpb-OH was converted to an amino derivative by attaching a diamino butane linker.
76. Synthesis of Monodisperse Macromolecular Bicyclic and Dendritic Compounds from (R)-3-Hydroxybutanoic Acid and Benzene-1,3,5-tricarboxylic Acid and Analysis by Fragmenting MALDI-TOF Mass Spectroscopy
Seebach, Dieter,Herrmann, Guido F.,Lengweiler, Urs D.,Amrein, Walter
, p. 989 - 1026 (2007/10/03)
As previously shown, oligo- and poly(β-hydroxyalkanoates) have a high tendency to form lamellar crystallites with ca. 50-A thickness which corresponds to chain lengths of 16 units (Fig. 1). To have monodisperse model compounds, we have now prepared bicyclic derivatives with three parallel (27-29) or two parallel and an antiparallel chain (68-70) consisting of up to 16 3-hydroxybutanoate (3-HB) units. We also prepared dendritic compounds (71-75, 82-85) containing oligo(3-HB) chains which cannot possibly he arranged as in the lamellae; the branching units were prepared from trimesic acid (= benzene-1,3,5-tricarboxylic acid). So far, none of the prepared samples formed crystals or contained crystalline domains which would have been suitable for single-crystal or powder-diffraction X-ray analysis. The terminally deprotected dendrimers (74, 75, and 85) are multi-anionic (up to 12 peripheral CO2H groups) and biodegradable. The macromolecular HB derivatives (molecular weight up to 10150 Da) have been fully characterized by IR, 1H- and 13C-NMR, [α]D, and elemental analysis. Especially important is the analysis by mass spectrometry with the MALDI-TOF technique (Fig. 2), proving that the products are monodisperse; application of a new variation of this MS method (post source decay = PSD or fragment analysis by structural time of night = FAST) allows for the observation of metastable fragment ions and, thus, is a tool for structural oligomer analysis (Fig. 3).
Regiospecific synthesis of 3,5-bis(bromomethyl)benzoic acid, a cysteine crosslinking agent
Engel,Burris,Slate,Erickson
, p. 8761 - 8770 (2007/10/02)
Bridging two molecules of an organic thiol with the 3,5-dimethylenebenzoic acid (Dmb) group produces a rigid five-carbon Dmb crosslink that is stable to disulfide reducing agents. Radical bromination of 3,5-dimethylbenzoic acid or its succinimido ester gave four α-brominated products. So NMR-pure 3,5-bis(bromomethyl)benzoic acid (Br2Dmb) was regiospecifically synthesized in 38% overall yield by a four-step route from 1,3,5-benzenetricarboxylic acid. S-Alkylation of cysteine methyl ester, a model thiol, with Br2Dmb provided the 2:1 adduct (Cys-OCH3)2Dmb in 79% yield. Subsequent N-protection with di(tert-butyl) dicarbonate gave (Boc-Cys-OCH3)2Dmb in 60% overall yield from cysteine methyl ester. This protected diamino acid is suitable for assembly of two Dmb-crosslinked peptide chains.
