- Identification of amino acid appended acridines as potential leads to anti-cancer drugs
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In order to develop the amino acid appended acridines as potential leads for anticancer drugs, they were subjected to preliminary investigations. Screening through MTT assay as well as the phase contrast micrographs and Confocal images of immunostained C6
- Singh, Palwinder,Kumar, Arun,Sharma, Anuradha,Kaur, Gurcharan
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Read Online
- Integrating Display and Delivery Functionality with a Cell Penetrating Peptide Mimic as a Scaffold for Intracellular Multivalent Multitargeting
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The construction of a multivalent ligand is an effective way to increase affinity and selectivity toward biomolecular targets with multiple-ligand binding sites. Adopting this strategy, we used a known cell-penetrating peptide (CPP) mimic as a scaffold to
- Bai, Yugang,Nguyen, Lien,Song, Ziyuan,Peng, Shaohong,Lee, Juyeon,Zheng, Nan,Kapoor, Iti,Hagler, Lauren D.,Cai, Kaimin,Cheng, Jianjun,Chan, H. Y. Edwin,Zimmerman, Steven C.
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Read Online
- Stitching of tyrosine and 10H-acridin-9-one: Turn-ON fluorescence in the narrow pH range 7.4-8.5 and intracellular labelling of cancer cells
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We tailored 10H-acridin-9-one and (S)-tyrosine into 3-(4-hydroxyphenyl)-2-[(9-oxo-9,10-dihydroacridine-4-carbonyl) amino]propionic acid (2). 2 underwent pH dependent protonation/deprotonation and the effect was harnessed in terms of change in the fluoresc
- Singh, Palwinder,Kumar, Arun,Kaur, Sukhmeet,Singh, Amrinder,Gupta, Muskan,Kaur, Gurcharan
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Read Online
- Synthesis, in vitro acetylcholinesterase inhibitory activity and molecular docking of new acridine-coumarin hybrids
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A novel series of acridine-coumarin hybrids was synthesized and biologically evaluated for their potential inhibitory effect on both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). The newly synthesized derivatives 9a–d have shown higher ac
- Hamulakova, Slavka,Janovec, Ladislav,Soukup, Ondrej,Jun, Daniel,Kuca, Kamil
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Read Online
- Solvothermal synthesis, structure, and fluorescence properties of three d10 polymers assembled from semi-rigid V-shaped aza-bridged multicarboxylate
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Hydro(solvo)thermal reactions between a new flexible multicarboxylate ligand, 2,2′-azanediyldibenzoic acid (H2L), and M(OH)2 (M = Cd, Zn) in the presence of different N-donor ancillary ligands, 4,4′-bipyridine (bpy) and pyridine (py)
- Tan, Yu-Hui,Xiong, Jian-Bo,Gao, Ji-Xing,Xu, Qing,Fu, Chao-Wu,Tang, Yun-Zhi,Yang, Shao-Ping,Wen, He-Rui,Shu, Qing
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Read Online
- N-Heterocyclic carbene (NHC)-catalyzed intramolecular benzoin condensation-oxidation
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NHC-Catalyzed intramolecular benzoin condensation-oxidation is developed for the expedient synthesis of diverse cyclic 1,2-diketones incorporated in dibenzo-fused seven-membered heterocycles in good to excellent yields, under ambient conditions. The prese
- Satyam, Killari,Ramarao, Jakkula,Suresh, Surisetti
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supporting information
p. 1488 - 1492
(2021/03/01)
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- Bis-aroylhydrazone based on 2,2′-bis substituted diphenylamine for synthesis of new binuclear organotin (IV) complexes: Spectroscopic characterization, crystal structures, in vitro DNA-binding, plasmid DNA cleavage, PCR and cytotoxicity against MCF7 cell
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New dinuclear organotin (IV) complexes, Me4Sn2L, Ph4Sn2L and Bu4Sn2L, have been synthesized from reaction of R2SnCl2 (R?=?Me, Ph and Bu) with a 2,2′-bis-substituted di
- Sedaghat, Tahereh,Shafiei, Mohammad,Simpson, Jim,Yousefi, Maryam
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- Bis-substituted diphenylamine arylidene hydrazones for the synthesis of new binuclear organotin(IV) complexes: Crystal structure, DNA cleavage and molecular docking
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Five dinuclear organotin(IV) complexes, R4Sn2La (R = Me, Ph) and R4Sn2Lb (R = Me, Ph and Bu) have been synthesized from reaction of R2SnCl2 with 2,4′- and 2,2′-bis-sub
- Yousefi, Maryam,Sedaghat, Tahereh,Simpson, Jim,Motamedi, Hossein,Dayer, Mohammad Reza
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p. 153 - 162
(2018/09/10)
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- COMPOUNDS FOR USE IN ORGANIC ELECTRONIC DEVICES
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A compound of formula (I): (Formula (I)) wherein Ar1, Ar2 and Ar3 independently in each occurrence is a C6-20 aryl group or a 5-20 membered heteroaryl group which is unsubstituted or substituted with one or more
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Page/Page column 21; 22
(2019/01/07)
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- Synthesis of Novel 4-acridonecarbohydrazide derivatives and their Antimicrobial Activities
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Synthesis of a library of twenty one 4-acridonecarbohydrazide was carried out under microwave-irradiations and there in-vitro antimicrobial activity were evaluated against different bacterial and fungal strain species. All twenty one derivatives were foun
- Manzoor, Mehwish,Perveen, Shahnaz,Tauseef, Saima,Jahan, Sitwat,Karim, Zahida,Karim, Aneela,Taha, Muhammad,Ismail, Nor Hadiani,Khan, Khalid Mohammed
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p. 405 - 413
(2017/06/27)
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- Design and synthesis of quinazolinone tagged acridones as cytotoxic agents and their effects on EGFR tyrosine kinase
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In a quest for finding potent cytotoxic molecules, we have designed and synthesized a new scaffold by tagging quinazolinones with an acridone moiety. The new acridone-4-carboximide derivatives were evaluated for their cytotoxic potentials against the MCF7 breast cancer cell line and three colon cancer cell lines (LS174T, SW1398, and WiDr). Compound 26 showed relatively potent cytotoxic activity among the derivatives, against all the cell lines tested. Mechanistic studies for the selected derivatives 7, 8, 16, 17, 25, and 26 were conducted through in vitro EGFR tyrosine kinase inhibition studies. The results indicate that compound 26 has a better EGFR tyrosine kinase inhibitory profile. The in vitro EGFR inhibition data was correlated with the cytotoxic properties, and molecular docking studies were performed with regard to the receptor autophosphorylation sites of the protein kinase domain of the EGFR.
- Babu, Yarlagadda Rajesh,Bhagavanraju, Mantripragada,Reddy, Gade Deepak,Peters, Godefridus J.,Prasad, Velivela V. S. Rajendra
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p. 624 - 634
(2014/11/08)
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- Synthesis, antiproliferative activity and tubulin targeting effect of acridinone and dioxophenothiazine derivatives
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The synthesis of new acridinone and dioxophenothiazine derivatives along with their tubulin polymerization inhibitory and antiproliferative activities is reported. The analysis of correlation for cytotoxic and antitubulin potential of tested compounds sho
- Verones, Valerie,Flouquet, Nathalie,Lecoeur, Marie,Lemoine, Amelie,Farce, Amaury,Baldeyrou, Brigitte,Mahieu, Christine,Wattez, Nicole,Lansiaux, Amelie,Goossens, Jean-Francois,Berthelot, Pascal,Lebegue, Nicolas
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- Developing bivalent ligands to target CUG triplet repeats, the causative agent of myotonic dystrophy type 1
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An expanded CUG repeat transcript (CUGexp) is the causative agent of myotonic dystrophy type 1 (DM1) by sequestering muscleblind-like 1 protein (MBNL1), a regulator of alternative splicing. On the basis of a ligand (1) that was previously reported to be active in an in vitro assay, we present the synthesis of a small library containing 10 dimeric ligands (4-13) that differ in length, composition, and attachment point of the linking chain. The oligoamino linkers gave a greater gain in affinity for CUG RNA and were more effective when compared to oligoether linkers. The most potent in vitro ligand (9) was shown to be aqueous-soluble and both cell- and nucleus-permeable, displaying almost complete dispersion of MBNL1 ribonuclear foci in a DM1 cell model. Direct evidence for the bioactivity of 9 was observed in its ability to disperse ribonuclear foci in individual live DM1 model cells using time-lapse confocal fluorescence microscopy.
- Jahromi, Amin Haghighat,Fu, Yuan,Miller, Kali A.,Nguyen, Lien,Luu, Long M.,Baranger, Anne M.,Zimmerman, Steven C.
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supporting information
p. 9471 - 9481
(2014/01/06)
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- Synthesis of novel heme-interacting acridone derivatives to prevent free heme-mediated protein oxidation and degradation
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Heme is an important prosthetic molecule for various hemoproteins and serves important function in living aerobic organisms. But degradation of hemoprotein, for example, hemoglobin during different pathological conditions leads to the release of heme, which is very toxic as it induces oxidative stress and inflammation due to its pro-oxidant nature. Thus, synthesis of compound that will detoxify free heme by interacting with it would be fruitful for the management of heme-induced pathogenesis. Here, we report the synthesis of a novel natural product arborinine and some other acridone derivatives, which interact with free heme. These acridones in vitro block heme-mediated protein oxidation and degradation, markers for heme-induced oxidative stress.
- Pal, Chinmay,Kundu, Milan Kumar,Bandyopadhyay, Uday,Adhikari, Susanta
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supporting information; scheme or table
p. 3563 - 3567
(2011/08/06)
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- Microwave-assisted synthesis and evaluation of substituted aryl propyl acridone-4-carboxamides as potential chemosensitizing agents for cancer
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A novel class of compounds with structure Aryl propyl acridone-4- carboxamides were synthesized by conventional and microwave (MW) irradiation methods and evaluated for their inhibitory effects on the transport activity of P- glycoprotein (P-gp) by standard Hoechst 33342 assay method. The title compounds with phenoxy substitution exhibited better activity.
- Velingkar, Vinaykumar S.,Dandekar, Vikrant D.
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p. 268 - 275
(2013/01/10)
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- Design, synthesis and evaluation of substituted N-(3-arylpropyl)-9,10- dihydro-9-oxoacridine-4-carboxamides as potent MDR reversal agents in cancer
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A novel class of molecules with structure N-(3-arylpropyl)-9,10-dihydro-9- oxoacridine-4-carboxamides (20-29) were designed by generating a pharmacophore for potent MDR reversal activity using phase drug design software. The designed molecules were synthesized by a novel synthesis route and evaluated for their inhibitory effects on the transport activity of P-glycoprotein (P-gp) by standard Hoechst 33342 assay method. Based on the pIC50 values of ten title compounds screened, three compounds exhibited better activity as compared to Verapamil used as standard.
- Velingkar,Dandekar
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experimental part
p. 504 - 510
(2012/01/06)
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- Targeting efflux pumps-In vitro investigations with acridone derivatives and identification of a lead molecule for MDR modulation
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To search multi drug resistance modulators, acridones carrying hydroxyl amine substituent at N-10 and COOH/Cl at C-4 were investigated for their interactions with the three components of efflux pump viz. P-gp, ATP, and Mg2+. Experimental and th
- Singh, Palwinder,Kaur, Jatinder,Yadav, Bhawna,Komath, Sneha Sudha
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experimental part
p. 4212 - 4223
(2010/09/12)
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- Design, synthesis and evaluations of acridone derivatives using Candida albicans-Search for MDR modulators led to the identification of an anti-candidiasis agent
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In order to search for MDR modulators, rationally designed acridone derivatives were investigated for their effect on influx or efflux of Rhodamine6G (R6G) in CAI4 cells. Results of these investigations indicate that in presence of compound 12, inhibition of growth of CAI4 cells and also an increased influx/efflux of R6G in CAI4 cells have been observed. This seems to be occurring due to the cell wall rupturing of Candida albicans. Compound 12 may be a suitable candidate for candidiasis therapy.
- Singh, Palwinder,Kaur, Jatinder,Yadav, Bhawna,Komath, Sneha Sudha
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body text
p. 3973 - 3979
(2009/10/17)
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- Design, synthesis and evaluation of 4,5-di-substituted acridone ligands with high G-quadruplex affinity and selectivity, together with low toxicity to normal cells
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A series of 4,5-di-substituted acridones have been designed and synthesized. Several compounds show high affinity for telomeric G-quadruplex DNA in classical and competition FRET assays, together with low duplex DNA affinity, although they do not show activity in a telomerase assay or evidence of telomere shortening. They have low toxicity against a panel of cancer cell lines and a normal human fibroblast line, and produce potent senescence-based long-term growth arrest in the MCF7 and A549 cancer cell lines.
- Cuenca, Francisco,Moore, Michael J.B.,Johnson, Karin,Guyen, Berangere,De Cian, Anne,Neidle, Stephen
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supporting information; experimental part
p. 5109 - 5113
(2010/03/31)
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- 9-Amino acridines undergo reversible amine exchange reactions in water: Implications on their mechanism of action in vivo
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9-Amino substituted acridities undergo a reversible amine exchange reaction In water under near-physiological conditions via an unstable hemiaminal intermediate. This thermodynamically controlled reaction may have Implications In understanding the mode of
- Paul, Alexis,Ladame, Sylvain
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supporting information; experimental part
p. 4894 - 4897
(2010/01/06)
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- Acridine-based agents with topoisomerase II activity inhibit pancreatic cancer cell proliferation and induce apoptosis
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A series of substituted 9-aminoacridines is evaluated for antiproliferative activity toward pancreatic cancer cells. The results indicate that the compounds inhibit cell proliferation by inducing a G1-S phase arrest. A model is also developed that explain
- Goodell, John R.,Ougolkov, Andrei V.,Hiasa, Hiroshi,Kaur, Harneet,Remmel, Rory,Billadeau, Daniel D.,Ferguson, David M.
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p. 179 - 182
(2008/09/17)
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- New acridone-4-carboxylic acid derivatives as potential inhibitors of Hepatitis C virus infection
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A new class of compounds-acridone derivatives-was tested using the direct fluorometric helicase activity assay to determine the inhibitory properties of the derivatives towards the NS3 helicase of Hepatitis C virus (HCV). The compounds were also tested as
- Stankiewicz-Drogon, Anna,Palchykovska, Larisa G.,Kostina, Valentina G.,Alexeeva, Inna V.,Shved, Anatoly D.,Boguszewska-Chachulska, Anna M.
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experimental part
p. 8846 - 8852
(2009/04/11)
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- Acridone derivatives: Design, synthesis, and inhibition of breast cancer resistance protein ABCG2
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The breast cancer resistance protein (BCRP, ABCG2) is among the latest discovered ABC proteins to be involved in MDR phenotype and for which only few inhibitors are known. In continuing our program aimed at discovering efficient multidrug resistance modul
- Boumendjel, Ahcene,Macalou, Sira,Ahmed-Belkacem, Abdelhakim,Blanc, Madeleine,Di Pietro, Attilio
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p. 2892 - 2897
(2007/10/03)
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- Fast synthesis of substituted N-phenylanthranilic acids using Ullmann condensation under microwave irradiation in dry media
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Substituted N-phenylanthranilic acids using the Ullmann condensation under microwave irradiation in dry media were obtained in good yield and short reaction times. Copyright Taylor & Francis LLC.
- Martin, Ana,Mesa, Miriam,Docampo, Maite L.,Gomez, Victoria,Pellon, Rolando F.
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p. 271 - 277
(2007/10/03)
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- Synthesis and evaluation of acridine- and acridone-based anti-herpes agents with topoisomerase activity
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The discovery of new non-nucleoside antiviral compounds is of significant and growing interest for treating herpes virus infections due to the emergence of nucleoside-resistant strains. Using a whole cell virus-induced cytopathogenic assay, we tested a se
- Goodell, John R.,Madhok, Avni A.,Hiasa, Hiroshi,Ferguson, David M.
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p. 5467 - 5480
(2007/10/03)
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- Identification of compounds with anti-West Nile virus activity
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The lack of antiviral compounds targeting flaviviruses represents a significant problem in the development of strategies for treating West Nile Virus (WNV), Dengue, and Yellow Fever infections. Using WNV high-throughput screening techniques developed in o
- Goodell, John R.,Puig-Basagoiti, Francesc,Forshey, Brett M.,Shi, Pei-Yong,Ferguson, David M.
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p. 2127 - 2137
(2007/10/03)
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- Microwave-assisted synthesis of N-phenylanthranilic acids in water
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N-Phenylanthranilic acid derivatives were synthesised using the Ullmann condensation of 2-chlorobenzoic acid with aniline derivatives under microwave irradiation in aqueous media. The method offers better yields in shorter reaction times compared to classical heating approaches using water as solvent.
- Martin, Ana,Pellon, Rolando F.,Mesa, Miriam,Docampo, Maite L.,Gomez, Victoria
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p. 561 - 563
(2007/10/03)
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- Synthetic studies on azacyclotribenzylenes
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Azacyclotribenzylene compounds (1, 2) and several of their N-alkyl derivatives (3-6) were synthesized via biarylamines (12, 14) in good yield. Conformational studies of them are also discussed.
- Hayashi, Kenta,Inoue, Shoko,Shimizu, Hanae,Kobayashi, Akiko,Ishizaki, Miyuki,Matsuoka, Yutaka,Nishitani, Kiyoshi,Hara, Hiroshi
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- Convenient access to substituted acridines by a Buchwald-Hartwig amination
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A convenient, high yield procedure for the synthesis of anthranilic acids carrying a variety of different substituents as well as their straightforward transformation into the corresponding 9-chloroacridines could be established by using modified Buchwald-Hartwig amination conditions.
- Csuk, René,Barthel, Alexander,Raschke, Christian
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p. 5737 - 5750
(2007/10/03)
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- Synthesis of C8-linked pyrrolo[2,1-c][1,4]benzodiazepine-acridone/acridine hybrids as potential DNA-binding agents
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Pyrrolobenzodiazepine hybrids linked to acridone/acridine ring systems at C8-position have been designed and prepared that exhibit significant DNA-binding affinity, and a representative compound shows promising in vitro anticancer activity.
- Kamal, Ahmed,Srinivas,Ramulu,Ramesh,Kumar, P. Praveen
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p. 4107 - 4111
(2007/10/03)
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- Synthesis of N-phenylanthranilic acid derivatives using water as solvent in the presence of ultrasound irradiation
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An improved synthesis of N-phenylanthranilic acid using water as solvent can be achieved by ultrasound irradiation. A number of N-phenylanthranilic acids were prepared in good yields in a very short reaction time.
- Docampo Palacios, Maite L.,Pellon Comdom, Rolando F.
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p. 1771 - 1775
(2007/10/03)
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- Synthesis and photophysics of acridine derivatives
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Highly fluorescent acridine derivatives were prepared by a multistep synthesis starting from 2-chlorobenzoic acid and the appropriate (aminophenyl)alkanoic acid by means of a modified Ullmann-Jourdan reaction followed by a cyclodehydration step, and by am
- Szymanska,Wiczk,Lankiewicz
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p. 801 - 808
(2007/10/03)
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- Synthesis and evaluation of anthranilic acid-based transthyretin amyloid fibril inhibitors
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Eight small molecules were synthesized to evaluate the structure activity relationships (SAR) of N-substituted anthranilic acids. The molecules were synthesized by benzylation or arylation of methyl anthranilate. A light scattering-based amyloid fibril formation assay was used to evaluate potential inhibitors of transthyretin (TTR) amyloid fibril formation in vitro. The m-carboxyphenylated and o-trifluoromethylphenylated anthranilic acids are potent inhibitors that will be subjected to further SAR and structural analysis.
- Oza, Vibha B.,Petrassi, H. Michael,Purkey, Hans E.,Kelly, Jeffery W.
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- Use of N,N-dimethylformamide as solvent in the synthesis of N-phenylanthranilic acids
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It is known that N-phenylanthranilic acids can be synthesized by Ullmann-Goldberg condensation in different conditions. This paper reports some parameters which influence the condensation and reports a general procedure for this reaction using N,N-Dimethylformamide as solvent.
- Pellon, Rolando F.,Carrasco, Ramon,Marquez, Tania,Mamposo, Taimirys
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p. 5107 - 5110
(2007/10/03)
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- Acridinecarboxamide compounds
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4-Carboxamidoacridine compounds represented by the general formula (I), STR1 where R1 represents H, CH3 or NHR3, where R3 is H, COCH3, SO2 CH3, COPh, SO2 Ph or lower alkyl optionally substituted with hydroxyl and/or amino functions; R2 represents H or up to two of the groups CH3, OCH3, halogen, CF3, NO2, NH2, NHCOCH3, and NHCOOCH3 placed at positions 1-3 or 5-8; Y represents C(NH)NH2, NHC(NH)NH2, or NR4 R5, where each of R4 and R5 is H or lower alkyl optionally substituted with hydroxyl and/or amino functions; and x is from 2 to 6, and the acid addition salts thereof, possess antibacterial and antitumor properties.
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