1,Phenanthroline forms a stable complex with Fe(II) ion called ferroin, which is used as an indicator in Fe(II) salt titrations. Ferroin is also. Structure, properties, spectra, suppliers and links for: phenanthroline, 1,Phenanthroline [ACD/Index Name] [ACD/IUPAC Name]. preferably any one of embodiments 1, 2 and 10, wherein ALK and ALK’ are both propylene, moetiy is typically an antagonist; if under such conditions the second targeting moiety is Tris(4,7-diphenyl- 1,phenanthroline)ruthenium( II).
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The conjugate of any one of embodiments 1 to 51wherein both the first adaptor moiety ADl and the second mmoetiy moiety AD2 are present.
It will be appreciated by a person skilled in the art that the various moieties of the conjugate of the invention are linked to or connected with each other by a linkage.
The preferred type of adapter moieties in one embodiment are amino acids, or activated forms thereof. In the following various design principles and reaction principles of an adapter moiety suitable for use in a conjugate of the invention will be outlined in the following.
Chemistryvolume 34, Inserted into a conjugate of the invention an adaptor moiety as preferably used in the conjugate of the invention is one which is indicated in the following formulae, whereby it is understood that to the extent the adapter moiety is represented in the formulae as being inserted between linking moiety LM and targeting moiety TM2 thus being a second adapter moiety, this is made for purpose of illustration only and the adapter moiety as such is the structure contained in square brackets.
Journal of Organometallic Chemistry.
Phenanthroline – Wikipedia
The conjugate of any one of embodiments 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14 and 15, preferably of any one of embodiments 12, 13, 14 and 15, wherein. The conjugate of any one of embodiments 2 to 55, wherein the Effector moiety is selected from the group comprising an Effector, Acceptor and -[Acceptor-Effector], wherein.
Due to the binding characterisitics of the conjugate of the invention it is also possible to target a first target targeted by the first targeting moiety and thus a cell, tissue and organ, respectively, expressing such first target, independently from the targeting of a second target targeted by the second targeting moiety and thus a cell, tissue and organ, respectively, expressing phenanthrolnie second target; and vice versa.
It is well understood that the synthesis of intermediates which contain said compound of formula 2 as a targeting moiety together with some other mowtiy as contained in the conjugate of the invention in activated form for further conjugation are of specific value by their own right.
It is within the present invention that a target to which the further targeting moiety of the conjugate of the invention is capable of phenanthrolins is a target that is expressed in an indication of group A as defined herein. Views Read Edit View history. The conjugate of any one of embodiments 2 to phenanthroljne, wherein the Phenanthrolie moiety EM is linked, preferably covalently linked to the branching moiety Y.
More preferably such discrimination or distinction forms the basis for said diagnosis and diagnosing, respectively. A C 1 -C 8 alkyl group can be unsubstituted or substituted with one or more groups, including, but not limited to, Ci- C 8 alkyl, [ C! In an embodiment of the conjugate of the invention the transporter to which the further targeting moiety of the conjugate of the invention is capable of binding, is selected from the group comprising an ATP -binding cassette transporter family, an F-type ATPase, a V-type ATPase, a P-type ATPase, a member of the major facilitator superfamily MFS of transporters, and a member of the SLC superfamily of solute carriers.
In a further embodiment of the conjugate of the invention a compound of formula 2in any of its embodiments, is present in the conjugate of the invention as targeting moiety TM2. Set,18, mostiy Cescato et al, J.
It performs very well for forming linkage to amino containing moieties bound to the solid phase resin. Accordingly, an adapter moiety is present in a conjugate of the invention in cases where two moieties of the conjugate of the invention do not provide reactive groups, more specifically, two addressable groups, i.
Examples of aryl pehnanthroline include, but are not limited to, phenyl, naphthyl and anthracenyl. The conjugate of any one of embodiments 20 and 21wherein the first targeting moiety is a compound of formula 4. One example for this is the attachment of a maleimide containing adapter moiety is described in example 5B:.
R 10 is selected from the group consisting of hydrogen and C! The conjugate of any one of embodiments 1, 2, 3, 4, 5 and 6, preferably any one of embodiments 1 and 2, wherein R is isopropyl. Acceptor is a moiety which mediates linking of an Effector to the third adapter moiety AD3, if present, or Acceptor is a moiety which mediates linking of an Effector to the branching moiety [Y], and.
O-Phenanthroline | C12H8N2 – PubChem
In an embodiment the conjugate of the invention is an antagonist to NTRl. Alternatively, sulfhydryl groups can be generated by reaction of an amino group of a lysine moiety of a targeting moiety using 2-iminothiolane Traut’s reagent or another sulfhydryl generating reagent.
Furthermore, a problem underlying the present invention is the provision of a kit which is suitable for use moetky any of the above methods. In an embodiment the phenxnthroline fish is shark.
It is within the present invention that a target to which the further targeting moiety of the conjugate of the invention is capable of binding, is a target that is expressed heterogeneously in an indication, preferably in an oncology indication, more preferably in any indication related to oncology.
The predominant response upon activation of the receptor by neurotensin is activation of phospholipase C, causing an increase in intracellular calcium levels. The affinity of neurotensin for the receptor could be decreased by both sodium ions and guanosine triphosphate GTP Vincent et al, Trends Pharmacol.
The conjugate of any one of embodiments 93 to 94, wherein the disease is selected from the group comprising tumors and hematological malignancies. In a perferred embodiment “a” and “b” are indivisually any integer from 1, 2, 3, 4 and 5. The anti-target with regard to the selectivity factor is preferably one which must not or should not be targeted by the further targeting moiety.
In a further embodiment of the conjugate of the invention the antibody is a human antibody, a humanized antibody, a chimeric antibody, a sub-primate antibody a murine antibody or an antibody from other species, i. The effector bearing agonist binds to the receptor and, upon binding to the receptor, the effector bearing agonist is internalized by the receptor and the effector bearing agonist thus trapped in the target cell.
As well-known from molecular-pharmacologic investigations efficient internalization is usually provided predominantly by agonists Bodei et ah, J. Simple alkyl chains wherein the two points of substitutions are in a maximal distance to each other like methane- 1,1-diyl, ethane- 1,2-diyl, propane- 1, 3 -diyl, butane- 1,4-diyl and pentane-l,5-diyl are also referred to as methylene which is also referred to as methane- 1,1 -diylethylene which is also referred to as ethane- 1 ,2-diylpropylene which is also referred to as propane- 1,3- diylbutylene which is also referred to as butane- 1,4-diyl and pentylene which is also referred to as pentane- 1,5 -diyl.
In an embodiment and as preferably used herein, an indication is a medical indication. This even more so in case such compound is moetly of a conjugate and wherein the conjugate comprises said compound targeting the receptor expressing tissues thus acting as a first targeting moiety, and a second compound capable of binding to a second target, whereby the second target may be, but does not have to be, different from the first target.
By contrast, neocuproine and bathocuproine form 1: The conjugate of any one of embodiments 1 to 78, for use in a method for the treatment of a disease.
The conjugate of any one of embodiments 1 to 26, preferably any one of embodiments 20 to 26, wherein the linker moiety LM is of general formula:. Alkyllithium reagents form deeply colored derivatives with phenanthroline. In a further embodiment of the conjugate of the invention the target-binding nucleic acid molecule is selected from the group comprising an aptamer Kang et al. In an embodiment and as preferably used herein, a diagnostically active compound is a compound which is suitable for or useful in the diagnosis of a disease.
Because of this, in a preferred embodiment an adaptor moiety provides for two reactive groups, whereby a first of said two reactive groups is suitable for generating a linkage between a first of the two moieties, and whereby a second of said two reactive groups is suitable for generating phenantnroline linkage between a second of phenantgroline two moieties. Only for colon weak or moderate expression under physiological conditions is described.
R 6 is selected from the group consisting of hydrogen and C!