scholarly journals Synthesis, Characterization And Antitumor Activity Of Copper(II) Complexes, [CuL2] [HL1-3=N,N-Diethyl-N'-(R-Benzoyl)Thiourea (R=H, o-Cl and p-NO2)]

2005 ◽  
Vol 3 (3-4) ◽  
pp. 299-316 ◽  
Author(s):  
Wilfredo Hernández ◽  
Evgenia Spodine ◽  
Lothar Beyer ◽  
Uwe Schröder ◽  
Rainer Richter ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Elemental Analysis ◽  
Copper Complexes ◽  
Mammary Adenocarcinoma ◽  
Molar Ratio ◽  
High Yield ◽  
Planar Geometry ◽  
Cytotoxic Activities ◽  
High Accumulation

The copper (II) complexes (CuL2) were prepared by reaction ofCu(CH3COO)2with the corresponding derivatives of acylthioureas in a Cu:HL molar ratio of 1:2. Acylthiourea ligands, N,N-diethyl-N'-(R-benzoyl) thiourea (HL1-3) [R=H, o-Cl and p-NO2] were synthesized in high yield (78-83%) and characterized by elemental analysis, infrared spectroscopy,1H and13C NMR spectroscopy. The complexes CuL2were characterized by elemental analysis, IR, FAB(+)-MS, magnetic susceptibility measurements, EPR and cyclic voltammetry. The crystal structure of the complex Cu(L2)2shows a nearly square-planar geometry with two deprotonated ligands (L) coordinated to CuIIthrough the oxygen and sulfur atoms in acisarrangement. The antitumor activity of the copper(II) complexes with acylthiourea ligands was evaluatedin vitroagainst the mouse mammary adenocarcinoma TA3 cell line. These complexes exhibited much higher cytotoxic activity (IC50values in the range of 3.9-6.9 μM) than their corresponding ligands (40-240 μM), which indicates that the coordination of the chelate ligands around the CuIIenhances the antitumor activity and, furthermore, this result confirmed that the participation of the nitro and chloro substituent groups in the complex activities is slightly relevant. The high accumulation of the complexes Cu(L2)2and Cu(L3)2in TA3 tumor cells and the much faster binding to cellular DNA than Cu(L1)2are consistent with thein vitrocytotoxic activities found for these copper complexes.

scholarly journals Studies on Synthesis of Aldimines: Part-I. Synthesis, Characterization and Biological Activity of Aldimines from Benzaldehyde with variedly substituted anilines

2018 ◽  
Author(s):  
C. J. Patil ◽  
Manisha C. Patil ◽  
Mrunmayee C. Patil
Keyword(s):  
Biological Activity ◽  
Aromatic Aldehyde ◽  
Elemental Analysis ◽  
High Purity ◽  
Aromatic Amines ◽  
Condensation Reaction ◽  
Physical Constant ◽  
High Yield ◽  
Substituted Anilines

A conventional condensation reaction of an aromatic aldehyde, Benzaldehyde with seven different aromatic amines viz. Aniline, 2-Choro-aniline, 3-Choro-aniline, 4-Choro-aniline, 2-Nitro-aniline, 3-Nitro-aniline and 4-Nitro-aniline and reacted efficiently to synthesize a series of Aldmines, I to VII, in moderate to high yield and high purity. The reaction was monitored and the products were analyzed by employing the TLC technique. All the products obtained were characterized by their colour, physical constant, TLC, elemental analysis and spectral (UV-Vis and FTIR) method. The synthesized Aldimines were subjected to in vitro biological activity.

Novel Meso-substituted Porphyrin Derivatives and its Potential use in Photodynamic Therapy of Cancer

2021 ◽  
Author(s):  
Pablo Vallecorsa ◽  
Gabriela Di Venosa ◽  
M. Belén Ballatore ◽  
Dario Ferreyra ◽  
Leandro Mamone ◽  
...  
Keyword(s):  
Photodynamic Therapy ◽  
Normal Skin ◽  
Hair Follicles ◽  
Systemic Administration ◽  
Mammary Adenocarcinoma ◽  
Quantum Yields ◽  
High Accumulation ◽  
Photodynamic Therapy Of Cancer ◽  
Potential Use

Abstract Background: Photodynamic therapy (PDT) is an anticancer treatment that utilizes the interaction of light and a photosensitiser (PS), promoting tumour cell death mediated by generation of reactive oxygen species. In this study, we evaluated the in vitro photoactivity of four meso-substituted porphyrins and a porphyrin coupled to a fullerene. Methods: The cell line employed was the LM3 mammary adenocarcinoma, and the PS with the best photokilling activity was administered to mice bearing the LM3 subcutaneously implanted adenocarcinoma. The TEMCP4+ porphyrin and its analogue TEMCC4+ chlorine contain four identical carbazoyl substituents at the meso positions of the tetrapyrrolic macrocycle and have A4 symmetry. The TAPP derivative also has A4 symmetry, and it is substituted at the meso positions by aminopropoxy groups. The DAPP molecule has ABAB symmetry with aminopropoxy and the trifluoromethyl substituents in trans positions. The TCP-C604+ dyad is formed by a porphyrin unit covalently attached to the fullerene C60.Results: The PSs are taken up by the cells with the following efficiency: TAPP> TEMCP4+= TEMCC4+> DAPP >TCP-C604+, and the amount of intracellular PS correlates fairly with the photodamage degree, but also the quantum yields of singlet oxygen influence the PDT outcome. TAPP, DAPP, TEMCC4+ and TEMCP4+ exhibit high photoactivity against LM3 mammary carcinoma cells, being TAPP the most active. After topical application of TAPP on the skin of mice bearing LM3 tumours, the molecule is localized mainly in the stratum corneum, and at a lower extent in hair follicles and sebaceous glands. Systemic administration of TAPP produces a tumour: normal skin ratio of 31.4, and high accumulation in intestine and lung.Conclusion: The results suggest a potential use of topical TAPP for the treatment of actinic keratosis and skin adnexal neoplasms. In addition, selectivity for tumour tissue after systemic administration highlights the selectivity of and potentiality of TAPP as a new PS.

scholarly journals Antitumor activity of new chemical compounds in triple negative mammary adenocarcinoma models

2020 ◽  
Vol 6 (3) ◽  
pp. FSOA442
Author(s):  
María V Giolito ◽  
Cristian M Camacho ◽  
Maitena Martinez-Amezaga ◽  
Carla I Traficante ◽  
Rocío A Giordano ◽  
...  
Keyword(s):  
Antitumor Activity ◽  
Tumor Cells ◽  
Anticancer Agents ◽  
Triple Negative ◽  
Chemical Compounds ◽  
Mammary Adenocarcinoma ◽  
Antitumor Action ◽  
Migratory Capacity ◽  
High Antitumor Activity

Aim: According to the need for the development of new anticancer agents, we have synthetized novel bioactive compounds and aimed to determine their antitumor action. Materials & methods: We describe in vitro studies evaluating the effect of 35 novel chemical compounds on two triple negative murine mammary adenocarcinoma tumors. Results & conclusion: Three compounds were selected because of their high antitumor activity and their low toxicity to normal cells. Their effect on tumor cells apoptosis, clonogenicity and migratory capacity, were determined. We found that the selected compounds showed inhibition of viability and clonogenic capacity, and promotion of apoptosis. They also decreased the migratory capacity of tumor cells. The results obtained suggest the likelihood of their future use as antitumor and/or antimetastatic agents.

Design, Syntheses and Biological Evaluation of 5-Fluoroindolin-2-One Derivatives with Urea Linkage

2013 ◽  
Vol 634-638 ◽  
pp. 926-929
Author(s):  
Bao Hua Zou ◽  
Zheng Fang ◽  
Zhao Yang ◽  
Kai Guo
Keyword(s):  
Antitumor Activity ◽  
1H Nmr ◽  
Elemental Analysis ◽  
Positive Control ◽  
Biological Evaluation ◽  
Antitumor Activities ◽  
Mtt Method ◽  
Antitumor Bioactivity ◽  
Better Than

Nine 5-fluoroindolin-2-one derivatives with urea linkage were designed and synthesized. The obtained structures were identified by 1H NMR, MS and elemental analysis. In vitro evaluation of antitumor bioactivity was performed by MTT method. Most of synthesized compounds showed antitumor activities, especially, compounds 6e and 6f, which were better than or equal to the antitumor activity of positive control.

scholarly journals Preparation, Characterization, and Antimicrobial Activities of Bimetallic Complexes of Sarcosine with Zn(II) and Sn(IV)

2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
Yasir Arafat ◽  
Saqib Ali ◽  
Saira Shahzadi ◽  
Muhammad Shahid
Keyword(s):  
Elemental Analysis ◽  
Zinc Acetate ◽  
Room Temperature ◽  
Antimicrobial Activities ◽  
Molar Ratio ◽  
Heterobimetallic Complexes ◽  
Nmr Data ◽  
Ft Ir ◽  
Coordinate Geometry

Heterobimetallic complexes of Zn(II) and Sn(IV) with sarcosine have been synthesized at room temperature under stirring conditions by the reaction of sarcosine and zinc acetate in 2 : 1 molar ratio followed by the stepwise addition of CS2and organotin(IV) halides, where R = Me,n-Bu, and Ph. The complexes were characterized by elemental analysis, FT-IR and NMR (1H,13C) spectroscopy. IR data showed that the ligand acts in a bidentate manner. NMR data revealed the four coordinate geometry in solution state.In vitroantimicrobial activities data showed that complexes (3) and (4) were effective against bacterial and fungal strains with few exceptions.

scholarly journals DNA Cleavage, Cytotoxic Activities, and Antimicrobial Studies of Ternary Copper(II) Complexes of Isoxazole Schiff Base and Heterocyclic Compounds

2014 ◽  
Vol 2014 ◽  
pp. 1-11 ◽  
Author(s):  
Vijay Kumar Chityala ◽  
K. Sathish Kumar ◽  
Ramesh Macha ◽  
Parthasarathy Tigulla ◽  
Shivaraj
Keyword(s):  
Antitumor Activity ◽  
Metal Complexes ◽  
Schiff Bases ◽  
Dna Cleavage ◽  
Spectral Studies ◽  
Planar Geometry ◽  
Cytotoxic Activities ◽  
Significant Activity ◽  
Antimicrobial Studies ◽  
Hela Cell Lines

Novel mixed ligand bivalent copper complexes [Cu. L. A. ClO4] and [Cu. L. A] where “L” is Schiff bases, namely 2-((3,4-dimethylisoxazol-5-ylimino)methyl)-4-bromophenol (DMIIMBP)/2-((3,4-dimethylisoxazol-5-ylimino)methyl)-4-chlorophenol (DMIIMCP), and “A” is heterocyclic compound, such as 1,10-phenanthroline (phen)/2,21-bipyridyl (bipy)/8-hydroxyquinoline (oxine)/5-chloro-8-hydroxyquinoline (5-Cl-oxine), have been synthesized. These complexes have been characterized by IR, UV-Vis, ESR, elemental analysis, magnetic moments, TG, and DTA. On the basis of spectral studies and analytical data, five-coordinated square pyramidal/four-coordinated square planar geometry is assigned to all complexes. The ligands and their ternary complexes with Cu(II) have been screened for antimicrobial activity against bacteria and fungi by paper disc method. The antimicrobial studies of Schiff bases and their metal complexes showed significant activity and further it is observed that the metal complexes showed more activity than corresponding Schiff bases. In vitro antitumor activity of Cu(II) complexes was assayed against human cervical carcinoma (HeLa) cancer cells and it was observed that few complexes exhibit good antitumor activity on HeLa cell lines. The DNA cleavage studies have also been carried out on pBR 322 and it is observed that these Cu(II) complexes are capable of cleaving supercoiled plasmid DNA in the presence of H2O2and UV light.

Phase I Study of a Liposomal Carrier (CPX-351) Containing an Optimized, Synergistic, Fixed Molar Ratio of Cytarabine (Ara-C) and Daunorubicin (DNR) in Advanced Leukemias and Myelodysplastic Syndromes (MDS).

Blood ◽  
2007 ◽  
Vol 110 (11) ◽  
pp. 900-900 ◽  
Author(s):  
Eric J. Feldman ◽  
Jeffrey E. Lancet ◽  
Jonathan E. Kolitz ◽  
Ekatherine Asatiani ◽  
Tania J. Curcio ◽  
...  
Keyword(s):  
Bone Marrow ◽  
Antitumor Activity ◽  
Dose Escalation ◽  
Phase 1 ◽  
Molar Ratio ◽  
Clinical Activity ◽  
Single Patient ◽  
Acute Leukemias ◽  
Grade 3

Abstract Background: The molar ratio of Ara-C and DNR profoundly affects the antitumor activity of this doublet in vitro. CPX-351 is a liposomal formulation of Ara-C and DNR which fixes the 5:1 molar ratio found to produce optimal synergy and efficacy in both in vitro and in vivo preclinical leukemia models, superior to that observed with conventionally dosed, non-encapsulated drugs. CPX-351 overcomes the individual pharmacokinetics of each drug maintaining the 5:1 molar ratio for extended periods of time after IV administration and delivers this ratio to bone marrow. We initiated an escalating-dose phase 1 trial of CPX-351 in patients with advanced acute leukemias or MDS. Objectives: 1) to determine safety, tolerability, and pharmacokinetics of a 3 day schedule (day 1, 3, 5) of CPX-351 in advanced leukemia and MDS, and 2) to seek preliminary evidence of antitumor activity. Methods: Patients with relapsed or refractory AML, ALL, or high-risk MDS were eligible for the study. 90 min. IV infusions of CPX-351 were administered on Days 1, 3, and 5 of each induction course. A second induction course was permitted if there was evidence of antileukemic effect and persistent leukemia in a day 14 bone marrow. Dose escalation began at 3 units/m2 (1 u = 1 mg Ara-C and 0.44 mg DNR) with single patient cohorts and doubling of doses with each cohort until evidence of antileukemic activity was observed. Thereafter, 3 patient cohorts and 33% dose increments were to be continued until DLTs signaled the end of further dose escalation. PK samples were collected after each dose. Results: Twenty-two subjects have received 31 courses of CPX-351: M/F = 15/7, median age = 62.5 years (range 24–78); 19 patients had AML and 3 patients had ALL; median number of prior regimens = 2 (1–7). At 24 u/m2 antileukemic effects were observed and future cohort size and escalation rate were adjusted (3 subjects/cohort, 33% dose increments). Non-hematologic toxicities observed to date have included transient grade 1–2 mucositis (5 patients), grade 2 skin rash (2 patients), grade 3 GI bleed (1 patient), and RSV pneumonia which resulted in death (1 patient). In addition, 6 subjects recovered from neutropenic fevers (5 grade 3) that were not considered study drug related. Except for a single patient treated at 24 u/m2, hair loss has not been observed. No DLT has been observed at doses up to 57 u/m2 (57 mg/m2 Ara-C/25 mg/m2 DNR). Clinical responses were observed beginning at 32 u/m2. At 32 u/m2 bone marrow aplasia occurred in 2 of 3 subjects with AML resulting in 1 CRp and 1 PR. At 43 u/m2 2 of 3 subjects achieved CR (1 AML, 1 ALL). Conclusions: CPX-351 administered on a 3x/week schedule in advanced leukemia appears to be well-tolerated, with preliminary and promising signs of clinical activity as measured by CR and decreases in bone marrow blasts. Accrual to this trial is ongoing, and updated clinical data will be presented.

scholarly journals Toxicity, Spectroscopic Characterization and Electrochemical Behaviour of New Macrocclic Complexes of Lead(II) and Palladium(II) Metals

2000 ◽  
Vol 7 (4) ◽  
pp. 211-218 ◽  
Author(s):  
Anil Bansal ◽  
Randhir Singh ◽  
R. V. Singh
Keyword(s):  
Electrochemical Behaviour ◽  
Macrocyclic Ligand ◽  
Pathogenic Fungi ◽  
Spectroscopic Characterization ◽  
Palladium Complexes ◽  
Molar Ratio ◽  
Azomethine Nitrogen ◽  
Planar Geometry ◽  
Template Process

Tetraazamacrocyclie complexes of lead and palladium have been synthesized by the template process using the bis(benzil)ethylenediamine precursor. The tetradentate macrocycle (maL) reacts with PbCl2, PdCl2 and different diamines in a 1:1:1 molar ratio in methanol to give several solid complexes of the types [Pb(maL)(R)Cl2] and [Pd(maL)(R)]Cl2 (where R = 2,6-diaminopyridine or 1,2-phenylenediamine). The macrocycle and its metal complexes have been characterized by elemental analysis, molecular weight determinations, molar conductivity, IR, 1H NMR, 13C NMR, electronic, mass and electrochemical studies. The macrocyclic ligand coordinates through the four azomethine nitrogen atoms which are bridged by benzil moieties. IR spectra suggest that the pyridine nitrogen is not coordinating. The palladium complexes exhibit tetracoordinated square-planar geometry, whereas a hexacoordinated octahedral geometry is suggested for lead complexes. The macrocycle along with its complexes have been screened in vitro against a number of pathogenic fungi and bacteria to assess their growth inhibiting potential.

scholarly journals Synthesis, biological evaluation, and molecular docking of ((4-([1,2,4]triazolo[4,3-b][1,2,4,5]tetrazin-6-yl) piperazin-1-yl)methyl) benzohydrazide derivatives

2020 ◽  
Vol 44 (9-10) ◽  
pp. 543-550
Author(s):  
Xiaoyu Wu ◽  
Feng Xu ◽  
Zhenzhen Yang ◽  
Zhonglu Ke ◽  
Lei Shi ◽  
...  
Keyword(s):  
Molecular Docking ◽  
Antitumor Activity ◽  
Tumor Cells ◽  
Elemental Analysis ◽  
Biological Evaluation ◽  
Significant Inhibition ◽  
Antitumor Activities ◽  
H Nmr ◽  
C Nmr

A series of ((4-([1,2,4]triazolo[4,3- b][1,2,4,5] methyl) benzo-hydrazide derivatives was designed, synthesized, and evaluated for their inhibition activities against five tumor cells and c-Met kinase in vitro. These compounds were fully characterized by 1H NMR, 13C NMR, MS, and elemental analysis. Antitumor experiments indicated that some compounds exhibited significant inhibition activities against A549 and Bewo. Especially, the IC50 values of 5f (12 μM), 5h (7.1 μM), 6a (8.4 μM), and 6d (9.2 μM) demonstrated better antitumor activities against A549 than the positive agent cisplatin (13.3 μM), and the IC50 value of 6a (5.2 μM) exhibited better antitumor activity against Bewo than cisplatin (7.7 μM).

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