A short and easy route is described for 6,8-disubstituted derivatives of quinoline 1,2,3,4-tetrahydroquinoli- ne from 6,8-dibromoquinolines 2 7 by various substitution reactions. While copper-promoted 6,8-dibromide produced monomethoxides 3 4, a prolonged reaction time mainly afforded dimethoxide 6 instead 5, whose aromatization with DDQ dibromide NaOMe in the presence CuI also gave rise to 6. Several quinolines were obtained treatment 6,8-dibromoquinoline (7) n-BuLi followed trapping an...

Abstract A series of substituted quinolines was screened for their antiproliferative, cytotoxic, antibacterial activities, DNA/protein binding affinity, and anticholinergic properties by using the 3‐(4,5‐dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide cell proliferation, lactate dehydrogenase cytotoxicity, microdilution assays, Wolfe–Shimmer equality method, Ellman esterase assay, respectively. The results cytotoxic anticancer activities compounds displayed that...

Due to a great deal of biological activities, quinoline derivatives have drawn attention for synthesis and activities in the search new anticancer drug development. In this work, variety substituted (phenyl, nitro, cyano, N-oxide, methoxy) (3-13) were tested vitro their activity against cancer cell lines, including rat glioblastoma (C6), human cervical cells (HeLa), adenocarcinoma (HT29). 6-Bromo-5-nitroquinoline (4), 6,8-diphenylquinoline (compound 13) showed greatest antiproliferative as...

This study uses a standardised protocol to explore prototype marmalade production using hawthorn fruit puree and sea buckthorn pectin. Hawthorn exhibited rich nutritional profile, prompting pectin incorporation enhance gelling capacity. Physicochemical analysis confirmed pectin's suitability. Evaluating gelation, influenced by Ca2+, identified optimal calcium lactate ranges. Samples underwent organoleptic assessment, showing appealing sensory attributes enhanced cavitation treatment....

Abstract 1-Indanone and its derivatives are well known for their diverse biological activities, making them valuable scaffolds in drug design medicinal chemistry. Among the various synthetic methodologies available modifying such structures, Suzuki-Miyaura cross-coupling reaction is a prominent approach constructing carbon-carbon bonds. In this study, palladium-catalyzed of 5-bromo-1-indanone with four different boronic acids—phenylboronic acid, 4-methoxyphenylboronic...

ABSTRACT In this study, we synthesized and characterized novel brominated methoxyquinolines ( 7 11 ) nitrated bromoquinoline 17 derivatives with potential antiproliferative activity against cancer cell lines. Starting from 1,2,3,4‐tetrahydroquinoline (THQ, 1 ), a series of quinoline compounds was obtained via regioselective bromination subsequent reactions. The structure the key compound, 3,5,6,7‐tetrabromo‐8‐methoxyquinoline confirmed using 1D 2D NMR techniques. Additionally, unexpected...

We report the synthesis of bromoindenoquinolines ( 15a – f ) by Friedlander reactions in low yields (13–50%) and conversion corresponding phenyl‐substituted indenoquinoline derivatives 16 21 high (80–96%) Suzuki coupling reactions. To explore structure–activity relationship (SAR), their inhibition potentials to inhibit acetylcholinesterase (AChE), butyrylcholinesterase (BChE), human carbonic anhydrase cyctosolic (hCA I II) enzymes were determined. Monophenyl 18 indenoquinolines significantly...

Abstract The aims of this study are to synthesize and characterize some new phenyl quinoline derivatives determine the activities them recently prepared substituted quinolines against Acetylcholinesterase (AChE) Charbonic anyhydrase (CA) enzymes microorganisms. 6‐phenyl‐ ( 3a ) 6,8‐diphenyl‐( 4a tetrahydroquinolines were by treatment 6‐bromo 6,8‐dibromo‐1,2,3,4‐tetrahydroquinoline with phenylboronic acids in presence Pd catalyze high yields respect our reported procedure. Then, bromination...

During the development of effective drugs for treatment cancer, one most important tasks is to identify drug candidates having maximum antiproliferation and minimum side effects. This paper considers problem selecting promising anticancer agents, showing inhibition at low IC50 concentration releasing lactate dehydrogenase percentage (cytotoxicity). Recently, we prepared quinoline analogs bearing different functional groups determined their potential against HeLa, C6, HT29 cancer cell lines...

Background: Brominated 8-hydroxy, 8-methoxy, 8-amino quinolines 5, 6, 8, 9 and novel cyano 8-hydroxyquinolines 11, 12 were evaluated in vitro for their anticancer effects on various cell lines. 5,7-Dibromo- 7-bromo- 7-cyano- 11 5,7-dicyano-12 shown to have strong antiproliferative activity against tumor lines, including C6 (rat brain tumor), HeLa (human cervix carcinoma), HT29 colon carcinoma) with IC50 values ranged from 6.7 25.6 µg/mL. Methods: A structure relationship (SAR) was conducted...

Abstract In this study, our goal was to synthesize novel aryl tacrine derivatives and assess their potential as anticancer, antibacterial agents, enzyme inhibitors. We adopted a two‐step approach, initiating with the synthesis of dibromotacrine 3 4 through Friedlander reaction. These intermediates underwent further transformation into diarylated 3a–e 4a–e using Suzuki–Miyaura cross‐coupling Thorough characterization these tacrines achieved various spectroscopic techniques. Our findings...

2,3'-Biindole (2) was synthesized via bromination of indole (1) with molecular bromine and underwent simultaneous dimerization. Antiproliferative cytotoxic activity 2 investigated in vitro on C6 (rat brain tumor), HeLa (human cervix carcinoma), HT29 colon carcinoma) cells lines by using BrdU cell proliferation ELISA lactate dehydrogenase (LDH) assays. In contrast to 5-fluorouracil (5-FU), 2,3'-biindole significantly inhibited lines. According LDH assay, the cytotoxicity compound low high...

Abstract The present study describes mono substituted indeno[1,2‐b]quinolines ( 3 a – c and 5 ) have much more antiproliferative potentials than positive controls against A549, HeLa, MCF7 Hep3B cell lines (IC 50 values 1.1–29.6 μg/mL) show similar cytotoxicity (14.3 % to 19.8 %) cells such as controls. Moreover, the indeno[1,2‐b]quinoline amines exhibit significant antimicrobial activity with MIC between 15.62 μg/mL 250 μg/mL. compounds can also bind DNA in groove binding mode constant range...

In this study, we developed a technology for the production of jelly confiture based on natural hawthorn puree. The use activated low-esterified pectin in recipe was shown to increase complexing ability product relation zinc and lead ions, making it suitable functional preventive nutrition. final characterised by bright orange-yellow colour, distinct taste odour, gelatinous consistency. Evaluation organoleptic, physicochemical, microbiological indicators showed that had high nutritional...

Abstract: Background: The inhibition of both hydrolysis products Acetylcholine (ACh), Acetylcholinesterase (AChE) and Butyrylcholinesterase (BChE), is essential for successful treatment Alzhemier patients. Objectives: This study was investigated potentials recently synthesized disubstituted tacrines derivatives on going our research against AChE, BChE carbonic anhydrase cyctosolic (hCA I II) enzymes to explore the Structure activity relationship (SAR). Methods: Inhibitory activities tested...