scholarly journals Synthesis and Spectroscopic and Biological Activities of Zn(II) Porphyrin with Oxygen Donors

2014 ◽  
Vol 2014 ◽  
pp. 1-13 ◽  
Author(s):  
Gauri Devi Bajju ◽  
Sujata Kundan ◽  
Madhulika Bhagat ◽  
Deepmala Gupta ◽  
Ashu Kapahi ◽  
...  
Keyword(s):  
Metal Ion ◽  
Human Cancer ◽  
Biological Activities ◽  
Thermal Studies ◽  
Blue Shift ◽  
Biological Evaluation ◽  
Axial Ligand ◽  
Molar Ratio ◽  
Central Metal

Results of investigation of the physicochemical properties of zinc complexes containing substituted phenols as axial ligand having general formula [X-Zn-t(p-CH3) PP] [where X = different phenolates as axial ligand] in impurity-free organic solvent are presented. The four-coordinated zinc porphyrin accepts one axial ligand in 1 : 1 molar ratio to form five-coordinated complex, which is purified by column chromatography and characterized by physicochemical, biological evaluation and TGA/DTA studies. Absorption spectra show two principal effects: a red shift for phenols bearing substituted electron releasing groups (−CH3, −NH2) and blue shift for phenols bearing electron withdrawing groups (−NO2, −Cl) relative to Zn-t(p-CH3) PP, respectively.1H NMR spectra show that the protons of the phenol ring axially attached to the central metal ion are merged with the protons of the porphyrin ring. Fluorescence spectra show two fluorescence peaks in the red region with emission ranging from 550 nm to 700 nm. IR spectra confirm the appearance of Zn-NPorand Zn-O vibrational frequencies, respectively. According to the thermal studies, the complexes have a higher thermal stability and the decomposition temperature of these complexes depends on the axial ligation. The respective complexes of X-ZnII-t(p-CH3) PP were found to possess higher antifungal activity (up to 90%) and higherin vitrocytotoxicity against human cancer cells lines.

scholarly journals Synthesis and Antimicrobial Studies of novel metal complexes of testosterone thiosemicarbazone and methandrostenolon thiosemicarbazone

2010 ◽  
Vol 4 (1) ◽  
pp. 73-84
Author(s):  
Redha I. Al-Bayati ◽  
Ahmed AbdulAmier ◽  
Hussain Al-Amiery ◽  
Yasmien K. Al-Majedy
Keyword(s):  
Metal Complexes ◽  
Metal Ion ◽  
Magnetic Moments ◽  
Antimicrobial Properties ◽  
Molar Ratio ◽  
Central Metal ◽  
Chemical Structures ◽  
Antimicrobial Studies ◽  
Number Of Microorganisms

This work involves the chemical synthesis of novel complexes derived from steroid hormones using testosterone and methandrostenolon as starting materials. When these starting materials react with thiosemicarbazide, L1 (testosteronthiosemicarbazone ) and L2 (methandrostenolonthiosemicarbazone ) are formed, and when they react with Cr (III), Co (II), Ni (II), and Cu (II) metal ions a new complexes are formed. The chemical structures for all the prepared compounds were characterized by elemental analysis, FT-IR, and UV/visible spectra. Moreover molar ratio M:L, metal content M%, and magnetic moments (μeff.) were also determined. The IR spectral data suggest the involvement of sulphur and azomethane nitrogen in coordination to the central metal ion. The free ligands and their metal complexes have been tested in vitro against a number of microorganisms (gram positive bacteria (Staphylococcus aureus), and gram negative bacteria (E. coli, Proteus vulgaris, Pseudomonas, and Klebsiella) in order to assess their antimicrobial properties. All the prepared complexes showed considerable activity against all bacteria.

scholarly journals Synthesis and Spectroscopic Studies of Axially Ligated Zn(II)5,10,15,20-meso-tetra(p-chlorophenyl)porphyrin with Oxygen and Nitrogen Donors

2013 ◽  
Vol 2013 ◽  
pp. 1-14 ◽  
Author(s):  
Gauri D. Bajju ◽  
Sujata Kundan ◽  
Ashu Kapahi ◽  
Deepmala Gupta
Keyword(s):  
Ir Spectra ◽  
Absorption Spectra ◽  
Elemental Analysis ◽  
Metal Ion ◽  
Electronic Absorption Spectra ◽  
Thermal Studies ◽  
Molar Ratio ◽  
Diffusion Method ◽  
Central Metal ◽  
H Nmr

Reaction of 5,10,15,20-meso-tetra(p-chlorophenyl)porphyrin[H2(p-Cl)pp] with zinc(II)acetate(Zn(OAc)2) and phenols results in the formation of corresponding axially ligated zinc(II)-meso-tetra(p-chlorophenyl)porphyrin (X-Zn-t(p-Cl)PP) (X = phenolates and pyridinates). The four-coordinated zinc porphyrin accepts one axial ligand in 1 : 1 molar ratio to form five-coordinated complex, which is purified by column chromatography and characterized by IR spectra,1H NMR, electronic absorption spectra, elemental analysis, mass spectroscopy, and TGA/DTA studies. IR spectra confirms the appearance of Zn– at 500–400 cm−1, Zn– at 650–570 cm−1and Zn–O at 650–350 cm−1.1H NMR spectra show that the protons of the Phenolic ring axially attached to the central metal ion are merged with the protons of the tetraphenyl rings of the porphyrin moiety. Absorption spectra reveal that complexes are accompanied by blue shift (hypsochromic shift) for phenolates and red shift (bathchromic shift) for pyridinates in comparison with the basic Zporphyrin emission bands. Mass Spectra determine them/zratio. The percentage of each element is confirmed by elemental analysis. According to the thermal studies, the complexes have a higher thermal stability and the decomposition temperature of these complexes depends on the axial ligation. Theinvitroantifungal activity of the complexes synthesized above had been done by disc diffusion method against the pathogen “Fusarium spp.,” which shows that with the increase in the concentration of the complexes, the colony diameter decreases and hence percent inhibition increases.

scholarly journals Study of Metal Complexes with Schiff Base Derived from 2-Amino-4, 6-dimethylbenzothiazole and Pyrrole-2- aldehyde

2021 ◽  
Vol 9 (VIII) ◽  
pp. 931-936
Author(s):  
Dr. Vilas G. Deshpande
Keyword(s):  
Metal Complexes ◽  
Spectral Data ◽  
Schiff Bases ◽  
Metal Ion ◽  
Thermal Studies ◽  
Analytical Data ◽  
Conductivity Measurement ◽  
Planar Geometry ◽  
Central Metal

As it is proved that the transition metal complexes have drug activities, hence we have synthesized heterocyclic Schiff bases. Six complexes of Co(II), Ni(II), Fe(III), Mn(II), Cr(II) and Cu(II) Schiff bases have been prepared. All ligands and its metal complexes the structures of the complexes have been proposed by analytical data, conductivity measurement, magnetic moment, IR, 1H NMR spectra and thermal studies. Analytical data confirmed 1:2 (metal:ligand) stoichiometry and the spectral data suggest that all Fe(III), Mn(II), Cr(II), Ni(II) and Co(II) complexes have octahedral geometry where as the Cu(II) metal complex shows the square planar geometry. The molar conductance values of metal complexes suggest their non electrolytic nature. The IR spectral data reveals that the ligand behaves as bidentate with O,N donor atoms sequence towards central metal ion. Antibacterial and antifungal activities of ligands and its metal complexes were performed in vitro against E.coli, S. typhi, S. aureus, B. subtilis and against various fungi like P.chrysogenum, A. niger, F. moniliformae, and A.Flavus. The complexes show more activity compare to the ligand.

Evaluation of Pyrano[3,2 C] Quinoline Analogues as Anticancer Agents

2019 ◽  
Vol 19 (10) ◽  
pp. 1285-1292 ◽  
Author(s):  
Kuldip D. Upadhyay ◽  
Anamik K. Shah
Keyword(s):  
Anticancer Agents ◽  
Human Cancer ◽  
Biological Activities ◽  
Cytotoxic Agents ◽  
Tumor Growth Inhibition ◽  
Mice Model ◽  
One Pot ◽  
Aryl Ring ◽  
Hct 116

Background: Quinoline analogues exhibited diversified biological activities depending on the structure type. A number of natural products with pyrano[3,2-c]quinolone structural motifs and patented chromenes were reported as promising cytotoxic agents. Objective: The present study is aimed to evaluate a new series of pyrano[3,2-c]quinoline scaffolds derived from the fusion of bioactive quinolone pharmacophore with structurally diverse aryl substituted chromene for its cytotoxicity. Methods: A library of pyrano[3,2-c]quinoline analogues was prepared from one-pot multi component synthesis using various aromatic aldehydes, malononitrile and 2,4-dihydroxy-1-methylquinoline. The new synthetics were primarily screened for its cytotoxicity (IC50) against different human cancer cell lines in vitro. The promising synthetics were further evaluated in vitro for their potency against different kinase activity. The promising compounds were finally tested for their in vivo efficacy in SCID type mice HCT-116 tumor model. Results: The screening results revealed that compounds 4c, 4f, 4i and 4j showed promising activity in in vitro study. However, compound 4c was found to be the most potent candidate with 23% tumor growth inhibition in HCT-116 tumor mice model. Conclusion: The structure activity relationship suggested that 3-substitution on the aryl ring at C4 position of the pyrano[3,2 c]quinolone moiety seems to have an important position for cytotoxicity activity. However, 3- chloro substitution at C4 aryl ring showed a significant alteration of the bioactive conformer of the parent scaffold and outcome with compound 4c as the most potent candidate of the series.

scholarly journals Hemisynthesis and Biological Evaluation of Cinnamylated, Benzylated, and Prenylated Dihydrochalcones from a Common Bio-Sourced Precursor

Antibiotics ◽  
2021 ◽  
Vol 10 (6) ◽  
pp. 620
Author(s):  
Anne Ardaillou ◽  
Jérôme Alsarraf ◽  
Jean Legault ◽  
François Simard ◽  
André Pichette
Keyword(s):  
Biological Activities ◽  
Biological Evaluation ◽  
Pharmacological Properties ◽  
Cytotoxic Potential ◽  
Naturally Occurring

Several families of naturally occurring C-alkylated dihydrochalcones display a broad range of biological activities, including antimicrobial and cytotoxic properties, depending on their alkylation sidechain. The catalytic Friedel–Crafts alkylation of the readily available aglycon moiety of neohesperidin dihydrochalcone was performed using cinnamyl, benzyl, and isoprenyl alcohols. This procedure provided a straightforward access to a series of derivatives that were structurally related to natural balsacones, uvaretin, and erioschalcones, respectively. The antibacterial and cytotoxic potential of these novel analogs was evaluated in vitro and highlighted some relations between the structure and the pharmacological properties of alkylated dihydrochalcones.

scholarly journals Green Synthesis andIn VitroBiological Evaluation of Heteroaryl Chalcones and Pyrazolines of Medicinal Interest

2013 ◽  
Vol 2013 ◽  
pp. 1-4 ◽  
Author(s):  
Vishal Banewar
Keyword(s):  
Green Synthesis ◽  
Elemental Analysis ◽  
Broad Spectrum ◽  
Spectroscopic Data ◽  
Heterocyclic Compounds ◽  
Biological Activities ◽  
Biological Evaluation ◽  
Active Compounds

Pyrazolines are well known and important nitrogen containing 5-membered heterocyclic compounds. In the present investigation, a series of various heteroaryl chalcones and pyrazolines were synthesized by condensing formylquinolines with diverse ketones. The newly synthesized 2-pyrazolines were characterized on the basis of elemental analysis and spectroscopic data. All of the newly synthesized target compounds were selected by the NCI forin vitrobiological evaluation. These active compounds exhibited broad spectrum of various biological activities. Most of the compounds showed potent activity.

scholarly journals SYNTHESIS AND ANTITUMOR ACTIVITY OF NEW MULTIFUNCTIONAL COUMARINS

2020 ◽  
Vol 17 (36) ◽  
pp. 871-883
Author(s):  
Moath Kahtan BASHIR ◽  
Yasser Fakri MUSTAFA ◽  
Mahmood Khudhayer OGLAH
Keyword(s):  
Schiff Base ◽  
Antitumor Activity ◽  
Human Cancer ◽  
Biological Activities ◽  
Cell Viability Assay ◽  
Chemical Structures ◽  
Viability Assay ◽  
Schiff Base Formation ◽  
Mcf 7

Cancer constitutes one of the most severe public health menaces worldwide. It is imperative to synthesize new compounds and explore their antitumor activity to find a potential resolution to this health problem. Synthesis of new scaffolds and evaluating their antitumor activity is a relevant approach for combating cancer development. Coumarins can exhibit diverse biological activities, and one of these is the antitumor activity. This study aimed to synthesize new coumarins by grafting their precursors to the aromatic amines via Schiff base formation and evaluating their introductory antitumor activity. New multifunctional coumarins (MC1-MC9) were prepared by integrating a functionalized coumarin with different toluidine derivatives via a Schiff-base linkage. Spectral characterization inspired by FTIR, 1H- and 13C- NMR spectroscopies has established the chemical structures of the synthesized products. The antitumor activity was explored in vitro versus four dominant human cancer lines, including HeLa, SKG, MCF-7, and AMN3. The outcomes acquired from the cell viability assay inspected by applying MTT dye have revealed that the synthesized multifunctional coumarins, particularly MC3, have a hopeful activity. It can be concluded that a similar trend of activity against the test cell lines was observed for the synthesized coumarins, with the best action being versus MCF-7 and the least one versus AMN3. This study not only affords a new scaffold of a significant antitumor activity but also provides some insights into its structureactivity relationship.

scholarly journals Isolation, Synthesis and Biological Evaluation of Phenylpropanoids from the Rhizomes of Alpania galanga

2013 ◽  
Vol 8 (12) ◽  
pp. 1934578X1300801 ◽  
Author(s):  
Sumit S Chourasiya ◽  
Eppakayala Sreedhar ◽  
K. Suresh Babu ◽  
Nagula Shankaraiah ◽  
V. Lakshma Nayak ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Colon Cancer ◽  
Anticancer Activity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Kinetic Resolution ◽  
Human Cancer ◽  
Cancer Cell Lines ◽  
Biological Evaluation

Bioactivity guided investigation of the DCM: MeOH (1:1) extract from the rhizomes of Alpinia galanga led to the isolation of phenylpropanoids (1–9) and their structures were established by 1H NMR, 13C NMR, IR and LC-MS/MS. These compounds have been evaluated for their in vitro anticancer activity against the human cancer cell lines A549 (lung cancer), Colo-205 (colon cancer), A431 (skin cancer), NCI H460 (lung cancer), PC-3 (prostate cancer), and HT-29 (colon cancer). Compounds 4 and 9 showed potent anticancer activity (ranging from 1.3–19.7 μg/mL) against all the tested cancer cell lines. In addition, an asymmetric synthesis of acetoxychavicol acetate (1) and trans-p-coumaryl alcohol (4) has been accomplished in six steps starting from readily available p-hydroxybenzaldehyde for the first time. Grignard reaction and Sharpless kinetic resolution reactions were utilized as the key steps to install the basic core.

scholarly journals SYNTHESIS, MOLLUSCICIDALAND ANTIMICROBIAL POTENTIALITIES OF IRON TRIAD MONONUCLEAR METAL COMPLEXES INCORPORATING TRIDENTATE ASYMMETRICAL SCHIFF BASE LIGANDS CONTAINING SOFT SULFUR COORDINATING ATOM

2019 ◽  
pp. 103-113
Author(s):  
AMAL M ALOSAIMI ◽  
INES EL MANNOUBI ◽  
SAMI A ZABIN
Keyword(s):  
Schiff Base ◽  
Metal Complexes ◽  
Metal Ion ◽  
Lethal Dose ◽  
Analytical Techniques ◽  
Central Metal ◽  
Schiff Base Ligands ◽  
Molluscicidal Activity

Objective: This work aimed at synthesizing tridentates asymmetrical Schiff base ligands containing sulfur atom and using them for preparing metal complexes with the iron triad metals. The prepared compounds were assayed in vitro for antimicrobial potential and in vivo molluscicidal activity. Methods: The unsymmetrical tridentate Schiff bases (SL1, SL2, and SL3) were prepared using 2-aminothiophenol as primary amine and condensed with 2-carboxybenzaldehyde, 2-hydroxy-1-naphthaldehyde, and 7-formyl-8-hydroxyquinoline. These ligands were used in preparing metal complexes with iron triad metals. The synthesized Schiff base ligands and their corresponding metal complexes were characterized and their proposed structures were confirmed using different physical and spectroscopic analytical techniques. All ligands and their corresponding metal complexes were assayed against different bacterial and fungal strains using the agar disk-diffusion technique. The molluscicidal activity was performed according to the standard reported methods as cited in the literature and by observing the toxicity and lethal dose according to the WHO guidelines. Results: The synthesized ligands behave as tridentate (NOS) ligands and form mononuclear complexes with the general formula [M(SL)2] with an octahedral geometry around the central metal ion. Metal complexes were non-electrolytic in nature. The in vitro antibacterial and antifungal examination results showed weak activity of the ligands, and there was enhanced activity with the complexes. The in vivo molluscicidal activity of the tested compounds showed good activity. Conclusion: The targeted compounds were prepared successfully, characterized, and showed some biological activity but lower than the standard reference drugs.

scholarly journals Distribution of Zinc in Mycelial Cells and Antioxidant and Anti-Inflammatory Activities of Mycelia Zinc Polysaccharides from Thelephora ganbajun TG-01

2020 ◽  
Vol 2020 ◽  
pp. 1-17
Author(s):  
Lan Zheng ◽  
Yaohong Ma ◽  
Yunjuan Zhang ◽  
Qingjun Meng ◽  
Junhui Yang ◽  
...  
Keyword(s):  
Biological Activities ◽  
Zinc Content ◽  
Helical Conformation ◽  
Molar Ratio ◽  
Oxygen Species ◽  
Zinc Supplement ◽  
Chronic Oxidative Stress ◽  
Main Fraction ◽  
Anti Inflammatory

This study demonstrates that Thelephora ganbajun had a strong ability to absorb zinc, and zinc can be compartmentally stored in the small vesicles and mainly accumulated in the form of zinc-enriched polysaccharides (zinc content was 25.0±1.27 mg/g). Mycelia zinc polysaccharides (MZPS) and its fractions were isolated. The main fraction (MZPS-2) with the highest antioxidant activity in vitro was composed of mannose : galacturonic acid : glucose : galactose in a molar ratio of 61.19 : 1 : 39.67 : 48.67, with a weight-averaged molecular weight of 5.118×105 Da. MZPS-2 had both α-pyranose and β-pyranose configuration and had a triple helical conformation. By establishing zebrafish models, we found that MZPS-2 can significantly scavenge free radicals, reduce the generation of reactive oxygen species caused by inflammation, and inhibit the recruitment of neutrophils toward the injury site. Therefore, MZPS-2 exhibited antioxidant and anti-inflammatory effects and can be used as a zinc supplement with specific biological activities to alleviate zinc deficiency complications, such as chronic oxidative stress or inflammation.

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