A FORMULATION INTENDED TO DISPLAY AN ANTI-CARCINOGENIC EFFECT BY AURORA A KINASE PHOSPHORYLATION SUPPRESSION
Creators: name: Alkoclar, Erdal Can
Publisher: name: Zenodo
Year: 2020
Subjects: Aurora A Kinase PGE-1

description: <strong>Field of Invention</strong> The present invention herewith discloses a formulation developed to display an anti-carcinogenic effect by aurora a kinase phosphorylation suppression. <strong>Background of the Related Technology</strong> At present it is known that phosphorylation is the reaction by which a phosphate group binds to an organic molecule. Phosphorylation is observed in five different ways. Oxidative phosphorylation is a metabolic path, by which ATP is formed by oxidation of nutrients. Phosphorylation is producing ATP in cells by using light energy. Phosphorylation in substrate level, is a chemical reaction where ATP is produced by transferring a phosphate group to ADP from a reactive intermediary product. Protein phosphorylation is having a phosphate group added to serine, threonine or tyrosine residues in protein which is mediated by a kinase enzyme. In chemistry ester of phosphoric acid is called organophosphate. In state of art technology, invention no “EP1746097B1", with title “1,4-dihydropyridine-fused heterocycles, process for preparing the same, use and compositions containing them” and under classification number “C07D 471/14" discloses 1,4-dihydropyridine fused heterocycles, process for preparing the same, use and compositions containing them. The referred invention is related to diydropyridine fused heterocycles where a beneficial substitution group is added for treatment of cancer and specifically to prevent division of cancer cells. These compounds act as Aurora A and/or Aurora B kinase inhibitors. Again invention no “EP2432766B1", with title “Anticancer compound and pharmaceutical composition containing the same" and under classification number “C07D 235/26" discloses a compound with formula (1): Preferably, this compound is in the form of a levorotatory compound (Ia). Particularly in methanol is has an optical rotation of [α]D= -38.6±0.7 at a concentration of 0.698 mg/ml. The compound is in the form of a base or an acid, specifically in the form of a pharmaceutically acceptable acid added salt. This compound is a selective inhibitor of Aurora A and B kinases. It can be used as an anti-cancer agent. Again invention no “EP1648426B1", with title “Benzimidazole derivatives and their use as protein kinases inhibitors" and under classification number “A61K 31/4184" relates compounds that act as inhibitors of Cyclin Dependent Kinases, Glycogen Synthase Kinases-3 and Aurora kinases, to the use of the compounds in the treatment of disease states or conditions mediated by the kinases. These compounds have general formula (I); where X is CR&lt;5&gt; or N; A, is a bond or -(CH<sub>2</sub>)m-(B)n-; B is C=O, NR(C=O) or O(C=O) where R is hydrogen or optionally hydroxy or C1-4 alkoxy substituted C1-4 hydrocarbyl; m is 0, 1 or 2; n is 0 or 1; R&lt;0&gt; is hydrogen or forms the -(CH2)p- group where, when exists, p is 2 to 4 together with NR; R&lt;1&gt; is hydrogen, a carbocyclic or heterocyclic group with 3-12 ring members or optionally substituted C1-8 hydrocarbyl group; R &lt;2&gt; is hydrogen, halogen, methoxy or optionally halogen, hydroxyl or methoxy substituted C1-4 hydrocarbyl group; R&lt;3&gt; and R&lt;4&gt; form a fused carbocyclic or heterocyclic ring optionally substituted, having 5 to 7 ring members and can be 3 heteroatoms selected from N, O and S together with the carbon atoms they are added and R&lt;5&gt; is hydrogen, one R&lt;2&gt; group or R&lt;10&gt;, where R&lt;10&gt; is halogen, hydroxy, trifluoromethyl, cyano, nitro, carboxy, amino, mono- or di-C1-4 hydrocarbylamino, carboxylic and heterocyclic group with 3-12 ring members, where R is a bond, O, CO, X&lt;1&gt;C(X&lt;2&gt;), C(X&lt;2&gt;)X&lt;1&gt;, X&lt;1&gt;C(X&lt;2&gt;)X&lt;1&gt;, S, SO, SO<sub>2</sub>, NR, SO<sub>2</sub>NR or NRSO<sub>2</sub> and an R-R group where R is, hydrogen, a carboxylic and heterocyclic group with 3-12 ring members and hydroxy, oxo, halogen, cyano, nitro, carboxy, amino, mono- or di-C1-4 hydrocarbylamino, a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from carbocyclic or heterocyclic groups with 3-12 ring members and where one or more carbon atoms of C1-8 hydrocarbyl group may be optionally substituted by O, S, SO, SO<sub>2</sub>, NR, X&lt;1&gt;C(X&lt;2&gt;), C(X&lt;2&gt;)X or X&lt;1&gt;C(X&lt;2&gt;)X&lt;1&gt;; R is hydrogen and is selected from C1-4 hydrocarbyl and X&lt;1&gt; is O, S or NR and X&lt;2&gt; is =O, =S or =NR. At the same time, the salts, solvates and N-oxides of the compound with formula (I) are also included. To conclude it has become inevitable to proceed with a development in the area of the related technology, considering the inadequacy of the existing solutions and the need for a formulation intended to display an anti-carcinogenic effect by aurora a kinase phosphorylation suppression. <strong>Objective of the Invention</strong> To overcome the disadvantages experienced in state of art technology; One objective of the invention is to suppress aurora A kinase phosphorylation. One other objective of the invention is to enhance pge-1 production The present invention which is aimed to achieve the above-mentioned advantages, is intended to display an anti-carcinogenic effect by aurora a kinase phosphorylation suppression and is a formulation that is obtained by combination of the compositions selected in a single form or in combinations from a group containing; 3,5,7-pentamethoxy-6-hydroxyloxane-2-yl]dioxyoxane-3-yl](E)-3-(3,4-hydroxyphenyl)prop-2-eneoate, 3,5,7-methoxy-6-hydroxyloxane-2-yl]dioxyoxane-3-tetracoumaroyl](E)-3-(3,4-methoxyphenyl)prop-4-eneoate. Structural and characteristic properties as well as all the advantages of the invention presented herewith will be clearly understood with the detailed description provided below and thus the evaluation regarding the present invention should be based on the detailed description presented herewith. <strong>Detailed Description of the Invention</strong> The present invention herewith discloses a formulation intended to display an anti-carcinogenic effect by aurora a kinase phosphorylation suppression. Referred formulation suppresses aurora A kinase phosphorylation, enhances pge-1 production. The formulation of the invention presented herewith contains; 3,5,7-pentamethoxy-6-hydroxyloxane-2-yl]dioxyoxane-3-yl](E)-3-(3,4-hydroxyphenyl)prop-2-eneoate, 3,5,7-methoxy-6-hydroxyloxane-2-yl]dioxyoxane-3-tetracoumaroyl](E)-3-(3,4-methoxyphenyl)prop-4-eneoate . The referred formulation is formed by mixing the above-mentioned components at below percentages by weight; 1-99% of 3,5,7-pentamethoxy-6-hydroxyloxane-2-yl]dioxyoxane-3-yl](E)-3-(3,4-hydroxyphenyl)prop-2-eneoate, 99-1% of 3,5,7-methoxy-6-hydroxyloxane-2-yl]dioxyoxane-3-tetracoumaroyl](E)-3-(3,4-methoxyphenyl)prop-4-eneoate. Components given above are obtained by combining the components from the above-mentioned group at the given range of weight ratios in a single form or in combinations thereof. The present invention at the same time discloses using the above-referred formulation intended to display an anti-carcinogenic effect by aurora a kinase phosphorylation suppression and manufacturing it for such purpose. <strong>CLAIMS</strong> A formulation intended to display an anti-carcinogenic effect by aurora a kinase phosphorylation suppression, which consists of combining the components selected from the group; 3,5,7-pentamethoxy-6-hydroxyloxane-2-yl]dioxyoxane-3-yl](E)-3-(3,4-hydroxyphenyl)prop-2-eneoate, 3,5,7-methoxy-6-hydroxyloxane-2-yl]dioxyoxane-3-tetracoumaroyl](E)-3-(3,4-methoxyphenyl)prop-4-eneoate in a single form or in combinations thereof. The formulation of Claim 1 which is characterized by containing 1-99% of 3,5,7-pentamethoxy-6-hydroxyloxane-2-yl]dioxyoxane-3-yl](E)-3-(3,4-hydroxyphenyl)prop-2-eneoate by weight. The formulation of Claim 1 which is characterized by containing 99-1% of 3,5,7-methoxy-6-hydroxyloxane-2-yl]dioxyoxane-3-tetracoumaroyl](E)-3-(3,4-methoxyphenyl)prop-4-eneoate by weight. Using the compositions obtained by selecting singly or in combination of components from the group of; 3,5,7-pentamethoxy-6-hydroxyloxane-2-yl]dioxyoxane-3-yl](E)-3-(3,4-hydroxyphenyl)prop-2-eneoate, 3,5,7-methoxy-6-hydroxyloxane-2-yl]dioxyoxane-3-tetracoumaroyl](E)-3-(3,4-methoxyphenyl) prop-4-eneoate from any one as given in Claims 2-3 in manufacturing the formulation intended to display an anti-carcinogenic effect by aurora a kinase phosphorylation suppression. <strong>SUMMARY</strong> <strong>A FORMULATION INTENDED TO HAVE AN ANTI-CARCINOGENIC EFFECT BY AURORA A KINASE PHOSPHORILATON SUPPRESSION</strong> <strong> </strong> The present invention herewith discloses a formulation intended to display an anti-carcinogenic effect by aurora a kinase phosphorylation suppression. Referred formulation suppresses aurora A kinase phosphorylation, enhances pge-1 production