Derivatives 3a-d Research Articles

Design, synthesis, molecular docking and DFT studies on novel melatonin and isatin based azole derivatives.

In order to address the pressing demand for newer broad-spectrum antifungal medicines with enhanced activity, computer modelling was utilised to rationally develop newer antifungal azole-based drugs. Based on the drug and active sites of the Lanosterol 14 alpha-Demethylases (LAD) of the prominent fungal pathogen Candida albicans interaction, Novel triazole-linked melatonin and isatin derivatives 7a-d and 8a-d were synthesised using bioisosterism. Besides the experimental synthesis and subsequent characterization, the present study focused on obtaining optimised geometries, frequency calculations, and TD-DFT studies of the synthesised molecules. We also performed molecular docking studies to explore the inhibitory ability of the synthesised compounds against the active sites of the Lanosterol 14 alpha-Demethylases (LAD) of the prominent fungal pathogen Candida albicans. The binding interactions resulted in positive findings, demonstrating the involvement of the synthesised compounds in the suppression of fungal growth. Comparative analysis of the binding potential of the synthesised molecules and commercially available drug fluconazole revealed a remarkable note: the docking scores for the designed drugs 7b, 7c, and 8c are much greater than those of the fluconazole molecule. The in silico study of the designed series of drug molecules serves as an important guideline for further exploration in the quest for potent antifungal agents.

Synthesis and Characterization of Novel Calix[4]arene Schiff Base Derivatives and Cytotoxicity Effect Evaluation on Cancer Cell Lines

In this study, four stages were used to create brand-new p-tert-butyl-calix [4] arene Schiff base derivatives. First, p-tert-butyl-phenol and formaldehyde are reacted to create p-tert-butyl-calix [4] arene (1). In the following step, methyl bromoacetate and p-ter-butyl-calix [4] arene (1) were combined with acetone and reflux to create the p-tert-butyl-calix [4] arene diester complex (2). The third step involves reacting the diester compound (2) and hydrazine hydrate to create the p-tert-butyl-calix [4] arene hydrazinamide molecule (3). In the final stage, calix [4] arene Schiff base derivatives (4a-d) were produced in good yields by combining compound (3), p-tert-butyl-calix [4] arene hydrazinamide, and various aldehyde derivatives with reflux in EtOH. Through the use of 1H-NMR, 13C-NMR, infrared spectroscopy, and elemental analysis, the structures of produced compounds were verified. Four distinct cancer lines are linked to the antitumor activity of synthetic chemicals. (HT-29, a human colon cancer cell line, PC-3, a human prostate cancer cell line, C6, a rat glioma cell line and MCF-7, a human breast cancer cell line). Weak antitumor activity was seen in synthetic substances. However, only compound 4b was found to have potential efficacy against C6 and HT-29. It is clear that compound 4b, which has a nitro substitute on the phenyl ring, draws attention due to its increased activity.

Design, synthesis and evaluation of novel Se-alkylated pyrazoles and their cyclized analogs as potential anticancer agents

A simple multicomponent reaction (MCR) was utilized to synthesize a series of 5-alkylated selanyl-1H-pyrazole derivatives 3a-d, 6a-d, and their 4-amino-5-substituted selenolo[2,3-c]pyrazole analogs (4a-d). The methodology is based on the substitution of selenium for the chlorine atom in the chloro pyrazole carbonitrile compound 1via reduction with sodium borohydride in a nitrogen atmosphere, followed by in-situ substitution reactions with various α-halo alkylating agents in the presence of a basic catalyst. The structures of the compounds were confirmed using elemental and spectroscopic techniques (FT-IR, 1H, 13C NMR, and mass spectrometry). The compounds were screened for their anticancer activity which showed promising results and compounds 4c and 6d exhibited the highest cytotoxicity against the HepG2 cell line with pIC50 values of 4.30 and 4.49 respectively, without showing any off-target toxicity. These molecules also, displayed good ADMET features, passed Lipinski's filters, showed good drug-likeness properties, and were predicted to be effective dual EGFR and VEGFR-2 inhibitors, causing downregulation of S100A4 and MMP-9 genes. Together, these results make these molecules as important lead molecules that could be studied further for their anticancer properties.

Synthesis, biological evaluation and molecular docking of new triphenylamine-linked pyridine, thiazole and pyrazole analogues as anticancer agents

A new series of pyridine, thiazole, and pyrazole analogues were synthesized. The pyridone analogues 4a-e were synthesized by treating N-aryl-2-cyano-3-(4-(diphenylamino)phenyl)acrylamides 3a-e with malononitrile. Many 4-arylidene-thiazolidin-5-one analogues 6a-d were obtained by Knoevenagel reactions of 4-(diphenylamino)benzaldehyde (1) with their corresponding thiazolidin-5-one derivatives 5a-d. The structural elucidation of the products was proven by the collections of spectroscopic methods such as IR, 1H NMR, 13C NMR, and MS data. Their anti-cancer activity was examined against two cell lines, MDA-MB-231 (mammary carcinomas) and A-549 (lung cancer). Compared with cisplatin as a reference standard drug, 6-amino-4-(4-(diphenylamino)phenyl)-2-oxo-1-(p-tolyl)-1,2-dihydropyridine-3,5-dicarbonitrile (4b) and 6-amino-4-(4-(diphenylamino)phenyl)-1-(4-nitrophenyl)-2-oxo-1,2-dihydropyridine-3,5-dicarbonitrile (4e) exhibited better efficiency against the A-549 cell line, with IC50 = 0.00803 and 0.0095 μM, respectively. Also, these compounds 4b and 4e showed the most potency among the examined compounds against MDA-MB-231 with IC50 = 0.0103 and 0.0147 μM, respectively. The newly synthesized compounds were docked inside the active sites of the selected proteins and were found to demonstrate proper binding. 2-Cyano-2-(4,4-(diphenylamino)benzylidene)-5-oxo-3-phenylthiazolidin-2-ylidene)-N-(p-tolyl)acetamide (6c) offered the highest binding affinity (− 8.1868 kcal/mol) when docked into (PDB ID:2ITO), in addition to 2-cyano-N-(4-(diethylamino)phenyl)-2-(4-(4-(diphenylamino)benzylidene)-5-oxo-3-phenylthiazolidin-2-ylidene)acetamide (6a) gave the highest energy score (− 9.3507 kcal/mol) with (PDB ID:2A4L).

Synthesis and preclinical evaluation of rhenium and technetium-99m “4 + 1” mixed-ligand complexes bearing quinazoline derivatives as potential EGFR imaging agents

Epidermal growth factor receptors (EGFR) of tyrosine kinase (TK) have shown high expression levels in most cancers and are considered a promising target for cancer diagnosis and therapy. Expanding the investigation for novel targeted radiopharmaceuticals, an EGFR inhibitor such as 4-aminoquinazoline derivatives along with a radionuclide such as technetium-99m (99mTc) could be ideal. Thus, we report herein the synthesis, characterization, and biological evaluation of new “4 + 1” mixed-ligand ReIII- and 99mTcIII-complexes of the general formula [99mTc][Tc(NS3)(CN-R)] bearing tris(2-mercaptoethyl)-amine (NS3) as the tetradentate tripodal ligand and a series of isocyanide derivatives (CN-R) of tyrosine kinase inhibitor (3-bromophenyl)quinazoline-4,6-diamine as the monodentate ligand. The quinazoline isocyanide derivatives 4a-d were prepared in two steps and reacted with the [Re(NS3)PMe2Ph] precursor leading to the final complexes 5a-d in high yield. All compounds were characterized by elemental analysis, IR, and NMR spectroscopies. In vitro studies, for their potency to inhibit the cell growth, using intact A431 cells indicate that the quinazoline derivatives 4a-d and the Re complexes 5a-d significantly inhibit the A431 cell growth. In addition, the EGFR autophosphorylation study of complex 5b shows an IC50 value in the nanomolar range.The corresponding “4 + 1” 99mTc-complexes 6a-d were prepared by employing the [99mTc]TcEDTA intermediate and the appropriate monodentate 4a-d in a two-step synthetic procedure with a radiochemical yield (RCY) from 63 to 77 % and a radiochemical purity (RCP) > 99 % after HPLC purification. Their structures have been established by HPLC comparative studies using the well-characterized Re-complexes 5a-d as reference. All 99mTc-complexes remain stable for at least 6 h, and their logD7.4 values confirmed their anticipated lipophilic character. Biodistribution studies in healthy Swiss albino mice of 99mTc-complexes showed hepatobiliary excretion and initial fast blood clearance. Complex 6b was also tested in Albino SCID mice bearing A431 tumors and showed rapid tumor uptake at 5 min (2.80 % ID/g) with a moderate tumor/muscle ratio (2.06) at 4 h p.i. The results encourage further investigation for this type of 99mTc-complexes as single-photon emission computed tomography (SPECT) radio agents for imaging tumors overexpressing EGFR.

Novel π-extended polycyclic chromenopyridines: Synthesis, DFT, electrochemical, and thermogravimetric evaluation

Polycyclic aromatic hydrocarbons (PAHs) doped with heteroatoms such as thiophene, carbazole, and boron-dipyrromethene (BODIPY) have attracted increased attention because of their excellent optoelectronic properties in addition to the robust skeletons required for the construction of efficient organic electronics. Herein, novel π-extended polycyclic chromenopyridines 3a-d, 5, and 7 were synthesized via base-catalyzed cascade reaction of 3-cyano-7,8-benzochromone 1 with acetonitrile derivatives 2a-d, ethyl chloroacetate 4, and phenylpyrazolone 6 in very good to excellent yields. Density functional theory (DFT) calculation and electrochemical evaluation of compounds 3a-d, 5, and 7 revealed a decreased energy gap (Eg) compared to the precursor 3-cyanochromone 1 indicating their superior semiconducting and light-harvesting abilities. In addition, the observed thermal stability of chromenopyridines 3a-d, 5, and 7 with maximum weight loss at temperatures between 301.72 and 557.28 °C qualified them for wide organic electronic applications.

Synthesis, biological activity and molecular docking study of some new chalcones, pyrazolines and isoxazolines derivatives bearing 1,2,3- triazoline

In this work a variety of new compounds such as chalcones, pyridine and isooxazoline derivatives has been synthesized. 2-((1-(4-acetylphenyl)-4,5-dihydro-1H-1,2,3-triazol-4-yl)methyl)benzo[d]isothiazol-3(2H)-one 1,1-dioxide(1) have been chosen as a starting material. Condensation of compound(1) with aromatic aldehydes namely benzaldehyde, p-chloro benzaldehyde, p-bromo benzaldehyde, p-nitro benzaldehyde, p-hydroxy benzaldehyde, m-hydroxy benzaldehyde, p-N,N-dimethyl benzaldehyde and 2,4-dimethoxy benzaldehyde in the presence of 40% KOH gave chalcone derivatives (2a-h). The cyclization of prepared chalcone derivatives semicarbazide in the presence acetic acid product pyrazoline derivatives(3a-f). Reaction of chalcone derivatives(2a-h) with hydroxylamine hydrochloride in the presence of sodium acetate afforded corresponding isooxazoline derivatives (4a-d). FT-IR, 1HNMR, and 13CNMR were used to characterize the target compounds. The results showed that the target compounds have a good biological activity such as antibacterial and antioxidant. The molecular docking studies of the target 6ul7 with the newly synthesized compounds showed good docking scores with acceptable binding interactions. The present results reveal that the newly synthesized compounds exhibit promising inhibition activity against Escherichia Coli.

Design, synthesis and biological evaluation of chromone derivatives as novel protein kinase CK2 inhibitors

Protein kinase CK2 is a potential target for the discovery of anticancer drugs. Flavonoids are reported to be effective CK2 inhibitors. Herein, based on structural trimming of flavonoids, a series of chromone-2-aminothiazole derivatives (1a-d, 2a-g, 4a-j, 5a-k) were designed and synthesized by hybridizing the chromone skeleton with 2-aminothiazole scaffold. Among these compounds, compound 5i was the most effective CK2 inhibitor (IC50 = 0.08 μM) and possessed potent anti-proliferative activity against HL-60 tumor cells (IC50 = 0.25 μM). Cellular thermal shift assay (CESTA) confirmed that 5i directly bound to the CK2, and the possible binding mode of 5i toward CK2 was also simulated. Further studies showed that 5i induced the apoptosis of HL-60 cells and arrested the cell cycle. Finally, western-blot analysis showed that 5i could inhibit the downstream of CK2, including α-catenin/Akt pathway and PARP/Survivin pathway.

A Facile and Efficient Synthesis of bis(Imidazo[1,2-a]pyridin-3-yl)methane and Vinyl Derivatives

An efficient synthetic route for the novel bis-imdizo[1,2-a]pyridine-3-yl)methane (2a-k) derivatives have been developed using acetic acid and two drops of trifluoroacetic acid at 40-45oC, resulting in 60-72% yields. An attempt to synthesize bis(Imidazo[1,2-a]pyridin-3-yl)methyl chloride derivatives by the reaction between two moles of imidazo[1,2-a]pyridine, one mole of chloroacetaldehyde in acetic acid, and two drops of trifluoroacetic acid was not successful, instead underwent dehydrohalogenation to yield vinyl derivatives (4a-d).

Antitrypanosomal activity of new semi-synthetic bergenin derivatives.

Bergenin and 11-O-(4'-O-methyl galloyl)-bergenin, previously isolated from Crassula capitella extract, were used as starting materials for the synthesis of eight derivatives; four derivatives 2a-2d were synthesized from bergenin through the formation of ester derivatives and four alkyl derivatives 4a-4d were synthesized from 11-O-(4'-O-methyl galloyl)-bergenin. The structures of the synthesized analogues were confirmed upon 1 H and 13 C NMR spectroscopic elucidation. Antileishmanial and antitrypanosomal activities of the synthesized derivatives were evaluated, compounds 11-O-(3',5' di-benzyl, 4'-O-methyl galloyl)-8,10-di-O-benzyl-bergenin (4c) and 11-O-(3',5'di-4-chlorobenzyl,4'-O-methyl galloyl)-8,10di-O-4-chlorobenzyl bergenin (4d) showed potent antitrypanosomal activity with IC50 values of 0.52 and 0.5μM, respectively and IC90 values of 0.66μM against T.brucei compared with IC50 and IC90 values of 21.7 and 50.3μM for the positive control difluoromethylornithine.

Green synthesis, cytotoxicity and antimicrobial activities of some new pyrazolines, pyrimidines and naphthyridines based on 1,3-di(thien-2-yl)prop-2-en-1-one using choline chloride-urea mixture as a deep eutectic solvent

An efficient and facile green synthesis of chalcone derivatives 1a-d was achieved by treatment of aromatic aldehydes with 2-acetylthiophene in the presence of choline chloride-urea mixture as a deep eutectic solvent. Chalcone 1a was used as a reactive key precursor to design a series of bio-active heterocycles such as pyrimidine, pyrazoline, pyridine, pyridopyrimidine and naphthyridine. The Structural formula of derivatives were confirmed and characterized by their elemental analyses and spectral data (IR, MS, 1H NMR, 13C NMR). In addition, the synthesized derivatives were evaluated for their antimicrobial activities, it was found that compounds 3, 8 and 9a exhibited potent antifungal activity in comparison with the standard drug. Cytotoxicity against breast cancer (MCF7) was screened also and most compounds showed low to moderate activity. The results of the viral screening against HBV of selected compounds indicated that compounds (9b, 15), 8, (3, 6), and 5 showed moderate viral replication inhibition.

Facile synthesis of some 5-(3-substituted-thiophene)-pyrimidine derivatives and their pharmacological and computational studies

A series of 5-(3-substituted-thiophene)-pyrimidine derivatives (3a-d) were synthesized via Knoevenagel condensation reaction in aq. ethanol using H2O2:HCl as a catalyst. Their pharmacological effects were evaluated. Analytical and spectroscopic methods confirmed the structures of the target molecules. The antibacterial activity studies revealed that compounds 3b and 3d exhibited the most effective zone of inhibition against bacterial strains E. coli and S. aureus, respectively. The in vitro cytotoxicity was carried out by MTT assay against MCF-7 cell line. The results showed excellent selectivity for all four compounds, among which the compound 3a exhibited remarkable cytotoxicity with a minimum cell viability range of 23.68 to 44.16%. The interaction of compounds with calf thymus DNA was determined using UV-absorption spectroscopy. The results confirmed that all the synthesized compounds interacted strongly with CT DNA through electrostatic or groove binding. In silico ADME-toxicology studies indicated that all the molecules under investigation are non-toxic with good oral bioavailability. The drug-likeness score indicated that they are suitable as drug-leads. In silico molecular docking the specified compound 3b bound with GlcN-6-P and P38 MAPk with a minimum binding energy of –7.9 and –6.4 kcal/mol, respectively. DFT study demonstrated that compound 3d was chemically and biologically more reactive due to less energy gap.

Benzofuran-oxadiazole hybrids: Design, Synthesis and antimicrobial activity studies

The six benzofuran-oxadiazole derivatives (4a-d) and (5a-b) have been designed, synthesized, characterized and evaluated for antimicrobial activity. The key synthetic intermediate 5-bromo-N'-hydroxybenzofuran -2-carboxamidine (3) was prepared from 5-bromobenzofuran-2-carboxylic acid (1) in two consecutive steps involving reaction with NaN3, in presence of TEA, Xtalfluor-E, PPh3 in dry DCM at 0oC followed by the treatment of resulting carbonitrile (2) with hydroxylamine hydrochloride in presence of sodium methoxide under reflux in aqueous ethanol. Reaction of carboxamidine (3) with different aryl esters in presence of K2CO3 under reflux conditions in toluene afforded 3-(5-bromobenzofuran-2-yl)-5-substituted phenyl-1,2,4-oxadiazoles (4a-d) while the refluxion of a solution of carboxamidine (3) in dichloromethane with chloro/bromo acetyl chloride in presence of TEA and a catalytic amount of HBTU furnished 3-(5-bromobenzofuran-2-yl)-5-(chloromethyl)-1,2,4-oxadia zole (5a) and 3-(5-bromobenzofuran-2-yl)-5-(bromomethyl)-1,2,4-oxadiazole (5b).

Synthesis and photophysical properties of benzimidazoles grafted pyrazole-containing pyrene or fluorene moiety: A combined spectroscopic and computational study

Herein, eight novel benzimidazoles grafted pyrazole-containing pyrene or fluorene moiety were synthesized. The substituent and solvent effects on the photophysical properties of the compounds have been analyzed based on their absorption and fluorescence bands in various solvents and the analysis was further supplemented by computational studies. The synthesized benzimidazoles derivatives show blue state emission in the range of 409–536 nm. Experimental absorption and emission wavelengths measured for all the synthesized benzimidazoles derivatives are in good agreement with those predicted using the Time-Dependent Density Functional Theory. The emission maxima of the methyl substituted compounds 6a-d increased compared to that of the unsubstituted derivatives 5a-d. However, upon methyl substitution the system undergoes fluorescence quenching. Computational analyses are used to understand the mechanism behind the fluorescence quenching and are helpful in explaining the electronic behavior of the chemical species reported here.

Synthesis, Structural Elucidation and Mesophase Behaviour of Hexasubstituted Cyclotriphosphazene Molecules with Amide Linking Unit

Alkylation of 4-acetamidophenol with various alkyl halides gave alkylated derivatives 1a-d which were further reduced to form amines, 2a-d. A separate reaction of phosphonitrilic chloride trimer and methyl-4-hydroxybenzoate yielded 3, hexa-(oxy-4-methyl benzoate)cyclotriphosphazene which was then reacted with ethanol and potassium hydroxide to give 4, hexa-(oxy-4-benzoic acid)cyclotriphosphazene. This hexasubstituted intermediate 4 was reacted with a series of intermediates 2a-d to yield the final compounds 5a-d, hexasubstituted cyclotriphosphazene with amide linking unit. All the structures of the intermediates and final compounds were characterized using Fourier Transform Infrared (FTIR) and Nuclear Magnetic Resonance (NMR) spectroscopy. The liquid crystal properties of all the synthesized compounds were determined using Polarized Optical Microscope (POM). POM observations showed that compounds 5a-d exhibited liquid crystal properties of smectic A and smectic C phases.

Synthesis and Anticonvulsant activity of new 5-((1-(2-(4-substituted phenacyl bromide)-2-oxoethyl)-2-phenyl-1H-indol-3yl) methylene) pyrimidine-2, 4, 6(1H, 3H, 5H)-trione Derivatives

In the current scenario we have plant to study to synthesize novel indole derivatives (4a-d) and (5a-b) which have the target activity like anti-convulsion and anti microbial etc. In the primary phase, we synthesized 2-phenyl-1H-indole reacted with Phosphorus oxychloride and N, N’-dimethylformamide by using vilsmeier reagent formylation of a new compound 2-phenylindole-3-carbaldehyde (2). The 2-phenylindole-3-carbaldehyde was reacted with substituted phenacyl bromide, K2CO3 and TBAB (Tetra butyl ammonium bromide) into the presence of N, N’-dimethylformamide to gives [1-(2-(4-substituted phenacyl bromide)-2-oxoethyl)-2-phenylindole-3-carbaldehyde (3a-d). The compound [1-(2-(4- substituted phenacyl bromide)-2-oxo-ethyl)-2-phenylindole-3-carbaldehyde was permitted to mixed with various substituted phenacyl bromide gives corresponding indole derivatives. The indole derivatives (3a-d) were reacted with barbituric acid and thiobarbituric acid dissolved into the methanol at reflux for 4h to gives afforded compounds (4a-d) and (5a-b). The final indole barbituric derivatives (4a-d) and (5a-b) were synthesized from substituted phenacyl bromide by the react with methanol and recrystalized from ethanol. The last compound has been completed on the basis of spectra FT-IR and 1H NMR. All the value of FT-IR, 1H NMR, Solubility and TLC were considered to be prominent. The pharmacological screening through ear electrode induced current 50mA for 0.2 seconds in electro-convulsiometer for anticonvulsant activity. The synthesize compounds were establish to be 4b, 4c, 4d, and 5a. The compound 4c and 5a were established to be the most potent compound through compare to standard drugs phenytoin sodium.

Novel benzenesulfonamides aryl and arylsulfone conjugates adopting tail/dual tail approaches: Synthesis, carbonic anhydrase inhibitory activity and molecular modeling studies.

New series of benzenesulfonamide and benzoic acid derivatives were designed and synthesized using tail/dual tail approach to improve potency and selectivity as carbonic anhydrase inhibitors. The synthesized compounds evaluated as CAIs against isoforms hCA I, II, IV and IX with acetazolamide (AAZ) as standard inhibitor. The benzenesulfonamide derivatives 7a-d, 8a-h, 12a-c, 13a and 15a-c showed moderate to potent inhibitory activity with selectivity toward isoform hCA II, especially, compound 13a with (Ki=7.6nM), while the benzoic acid analogues 12d-f, 13b and 15d-f didn't show any activity except compounds 12d,f and 15e that showed weak activity. Additionally, molecular docking was performed for compounds 7a, 8a, 8e, 12a, 13a and 15a on isoform hCA I, II to illustrate the possible interaction with the active site to justify the inhibitory activity.

Design, cytotoxic effects on breast cancer cell line (MDA-MB 231), and molecular docking of some maleimide-benzenesulfonamide derivatives

A group of novel maleimide-benzenesulfonamide derivatives 3a-d was designed and synthesized for their evaluation as a potential anti-breast cancer agent. The structures of these derivatives were confirmed by their 1H, 13C NMR, Mass, FT-IR spectral data, and melting points. The cytotoxic activity (in vitro) of the selected molecules against MDA-MB231 ​cell line was evaluated by MTT method. Among them, compounds 3a and 3d exhibited a significant cytotoxicity with the IC50 value of 1.61 and 1.26 ​μM, respectively, whereas compounds 3b and 3c showed a moderate cytotoxicity with IC50 values of 0.45 and 1.12 ​μM, respectively against MDA-MB231 ​cells. Docking modeling of the synthesized compounds 3a-d into binding sites of human aromatase protein (PDB ID: 4GL7) was performed to investigate if these derivatives possess analogous binding mode to breast cancer proteins. Docking results showed these compounds have efficient interactions such as hydrogen bonding, Van der Waals interactions, and hydrophobic interactions with the active site residues of the aromatase protein (PDB ID: 4GL7). The low binding energies and a number of hydrogen bonding indicated that the maleimide-benzenesulfonamide derivatives might be considered as a promising anti-breast cancer agent with further developments in drug discovery.

Utility of dipyrromethane in the synthesis of some new A2B2 porphyrin and their related porphyrin like derivatives with their evaluation as antimicrobial and antioxidant agents

In this work, the dipyrromethane derivatives 2a,b were synthesized from an aldehyde and excess of pyrrole at room temperature in solvent-free conditions. The reaction of dipyrromethanes 2a,b with different aromatic aldehydes in the presence of hydrochloric acid or p-toluenesulfonic acid as a catalyst afforded some new porphyrin like and A2B2 porphyrin derivatives 4a-g and 5a-d, respectively. Biological evaluation of the newly synthesized compounds 4a-g and 5a-d showed promising activity as antimicrobial and antioxidant agents. Compounds 4c,4e,4g,5c, and 5d exhibited the highest antimicrobial activity, whereas, compounds 4a,4f,5a,5b, and 5d recorded the highest antioxidant activity.

Cytotoxic and apoptotic potential of some coumarin and 2-amino-3-carbonitrile selenophene derivatives in prostate cancer.

3-acetyl coumarin derivatives (1a-d) are formed as a result of condensation of salicylaldehyde derivatives and ethyl acetoacetate and were converted into coumarin-selenophene hybrid compounds (2a-d) in the basic medium by modified Gewald reaction in the presence of malononitrile and selenium. Products are characterized by nuclear magnetic resonance (NMR). The prepared compounds are screened for their anticancer activity against DU-145 cell line. In addition, selected target compounds are evaluated for apoptosis and oxidative stress on DU-145 (prostate carcinoma) cell lines.