We report herein an innovative approach to prostate tumor therapy using tumor specific radioactive gold nanoparticles (198Au) functionalized with Mangiferin (MGF). Production and full characterization of MGF-198AuNPs are described. In vivo therapeutic efficacy of MGF-198AuNPs, through intratumoral delivery, in SCID mice bearing prostate tumor xenografts are described. Singular doses of the nano-radiopharmaceutical (MGF-198AuNPs) resulted in over 85% reduction of tumor volume as compared to untreated control groups. The excellent anti-tumor efficacy of MGF-198AuNPs are attributed to the retention of over 90% of the injected dose within tumors for long periods of time. The retention of MGF-198AuNPs is also rationalized in terms of the higher tumor metabolism of glucose which is present in the xanthanoid functionality of MGF. Limited/no lymphatic drainage of MGF-198AuNPs to various non-target organs is an attractive feature presenting realistic scope for the clinical translation of MGF-198AuNPs in for treating prostate cancers in human patients. The comparative analysis of MGF-198AuNPs with other radioactive gold nanoparticles, functionalized either with epigallocatechin gallate or the Gum Arabic, has revealed significantly superior tumoricidal characteristics of MGF-198AuNPs, thus corroborating the importance of the tumor-avid glucose motif of MGF. Oncological implications of MGF-198AuNPs as a new therapeutic agent for treating prostate and various solid tumors are presented.
New ligand of N-(pyrimidin-2-yl carbamothioyl)acetamide was synthesized and its complexes with (VO(II), Mn (II), Cu (II), Zn (II), Cd (II) and Hg (II) are formed with confirmation of their structures on the bases of spectroscopic analyses. Antimicrobial activity of new complexes are studied against Gram positive S. aureus and Gram negative E. coli, Proteus, Pseudomonas. The octahedral geometrical structures are proved depending on the outcomes from the preceding procedures
New Schiff base ligand (E)-6-(2-(4-(dimethylamino)benzylideneamino)-2-(4-hydroxyphenyl)acetamido)-3,3- dimethyl-7-oxo-4-thia-1- azabicyclo[3.2.0]heptane-2-carboxylic acid = (HL) was synthesized via condensation of Amoxicillin and 4(dimethylamino)benzaldehyde in methanol. Figure -1 Polydentate mixed ligand complexes were obtained from 1:1:2 molar ratio reactions with metal ions and HL, 2NA on reaction with MCl2 .nH2O salt yields complexes corresponding to the formulas [M(L)(NA)2Cl],where M=Fe(II),Co(II),Ni(II),Cu(II),and Zn(II), A=nicotinamide .
In :the _pr sent _paper we report ths. ynthesis ·of a new li:ga!!d..
[f4LJ [{'2 {1-'[(2-hyd•:0xy-.ben:zy1i.den·e)..,bxcJrazanci}:etby-l }benzerieÂ
J,5 t;rtiol .aad its complexes ·w-ith '('Mlif(1 J Fev 1 ), ed(J'l), and. :f.::I:g 01>-)
The ligand \VS preP..ated rin tWo steps' • fp I t}Je nrst stea -soJutiQil Qf
-saUcyla[deeyeq. ip methatt:oJ . re3ctcd lU1der reflux
... Show MoreEight different Dichloro(bis{2-[1-(4-R-phenyl)-1H-1,2,3-triazol-4-yl-κN3]pyridine-κN})iron(II) compounds, 2–9, have been synthesised and characterised, where group R=CH3 (L2), OCH3 (L3), COOH (L4), F (L5), Cl (L6), CN (L7), H (L8) and CF3 (L9). The single crystal X-ray structure was determined for the L3 which was complemented with Density Functional Theory calculations for all complexes. The structure exhibits a distorted octahedral geometry, with the two triazole ligands coordinated to the iron centre positioned in the equatorial plane and the two chloro atoms in the axial positions. The values of the FeII/III redox couple, observed at ca. −0.3 V versus Fc/ Fc+ for complexes 2–9, varied over a very small potential range of 0.05 V.
... Show MoreThe eaction of 2 4 .6-trihydroxyactophenonemonohydra1e with
l hydr.azine monohydrate was realized ti·nder reflu.(( in methanol and i:l.
Jew drops of glacial acetic acid we.re added to give lhe'(int rmediate)
2-(1hydr pno-ctbyt)-benzcne-·1.3.5-r:Qql, which reacted wittl
saEcy.laldehyde. jn methm)ql to gjy;e 'a new :tyRe CNzOi) Ligand (H:flL]
f(2-{1-[(2-=bydroxy-bertzylide·ne)-bydrazqoo,J-e·thy.1}bcnze·neJ ;3·,5
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New Schiff base [3-(3-acetylthioureido)pyrazine-2-carboxylic acid][L] has been prepared through 2 stages, the chloro acetyl chloride has been reacting with the ammonium thiocyanate in the initial phase for producing precursor [A], after that [A] has been reacting with the 3-amino pyrazine-2-carboxilic acid to provide a novel bidentate ligand [L], such ligand [L] has been reacting with certain metal ions in the Mn(II), VO(II), Ni(II), Co(II), Zn(II), Cu(II), Hg(II), and Cd(II) for providing series of new metal complexes regarding general molecular formula [M(L)2XY], in which; VO(II); X=SO4,Y=0, Co(II), Mn(II), Cu(II), Ni(II), Cd(II), Zn(II), and Hg(II); Y=Cl, X=Cl. Also, all the compounds were characterized through spectroscopic techniques [
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