Publications by authors named "Tarek Afifi"

In this study, novel selective antitumor compounds were synthesized based on their fundamental pharmacophoric prerequisites associated with EGFR inhibitors. A molecular hybridization approach was employed to design and prepare a range of 4-chromene-3-carboxylates -, , and - derivatives, each incorporating a sulfonamide moiety. The structures of these hybrid molecules were verified using comprehensive analytical and spectroscopic techniques.

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Background: The number of patients undergoing exchange of textured implants for smooth devices has greatly increased because of concern over breast implant-associated anaplastic large-cell lymphoma (BIA-ALCL). The authors examined long-term patient- and surgeon-reported outcomes in terms of aesthetics, comfort, and complications.

Methods: Patients who underwent reconstruction with shaped, textured implants replaced with round, smooth implants between 1994 and 2022 and who had a minimum follow-up of 1 year were included.

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Mushrooms possess antihyperglycemic effect on diabetic individuals due to their nonfibrous and fibrous bioactive compounds. This study aimed to reveal the effect of different types of mushrooms on plasma glucose level and gut microbiota composition in diabetic individuals. The effects of five different mushroom species (, GLM; , POM; , PCM; , LEM; or , HMM) on alloxan-induced diabetic rats were investigated in this study.

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-Enaminonitriles bearing 9-hydroxy-1-benzo[]chromene moiety was synthesized. The targeted compounds were evaluated for their anti-proliferative activity against three human tumor cell lines, PC-3, SKOV-3 and HeLa, and the active cytotoxic compounds were further evaluated against cancer cells, MCF-7/ADR, and two normal cell lines, HFL-1 and WI-38. Few compounds were assigned to be the most potent derivatives against PC-3, SKOV-3 and HeLa cell lines in comparison with Vinblastine and Doxorubicin.

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Background: Molecules bearing an active methylene bridge are one of the most fruitful and remarkable precursors that have been incorporated into the synthetic strategy of an assortment of bioactive compounds.

Objective: The reactive methylene derivatives have been endowed with multiple reactions, which target biological and medicinal applications and result from their structural diversity and discrete reactivity.

Methods: The present report endeavors to synthesize, characterize, and in-vitro evaluate several novel propanoic acids, coumarin, and pyrazole derivatives as antimicrobial and antiproliferative agents.

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The predominant impediments to cutaneous wound regeneration are hemorrhage and bacterial infections that lead to extensive inflammation with lethal impact. We thus developed a series of composite sponges based on polyvinyl alcohol (PVA) inspired by marjoram essential oil and kaolin (PVA/marjoram/kaolin), adopting a freeze-thaw method to treat irregular wounds by thwarting lethal bleeding and microbial infections. Microstructure analyses manifested three-dimensional interconnected porous structures for PVA/marjoram/kaolin.

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Maxillonasal dysplasia or Binder syndrome is an uncommon condition. It is a congenital disease characterized by undergrowth of the central face and may include elements of the nose and upper jaw. The hallmark of the deformity is a retruded mid-face and an extremely flat nose.

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Article Synopsis
  • Selenium-containing heterocyclic compounds, particularly new pyridine derivatives, have become a focus of interest for their potential as bioactive molecules with antimicrobial properties.
  • A one-pot multicomponent approach using solvent-free microwave irradiation was utilized for their synthesis, with spectroscopic techniques confirming the structures of the compounds.
  • Antimicrobial activity was tested via the agar diffusion method, revealing some derivatives showing significant antibacterial and antifungal activity, particularly one that demonstrated the strongest performance, supported by molecular docking and DFT calculations for further insights into molecular geometry and reactivity.
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The high biological activity of the chromene compounds coupled with the intriguing optical features of azo chromophores prompted our desire to construct novel derivatives of chromene incorporating azo moieties 4a-l, which have been prepared via a three-component reaction of 1-naphthalenol-4-[(4-ethoxyphenyl) azo], 1, with the benzaldehyde derivatives and malononitrile. The structural identities of the azo-chromene 4a-l were confirmed on the basis of their spectral data and elemental analysis, and a UV-visible study was performed in a Dimethylformamide (DMF) solution for these molecules. Additionally, the antimicrobial activity was investigated against four human pathogens (Gram-positive and Gram-negative bacteria) and four fungi, employing an agar well diffusion method, with their minimum inhibitory concentrations being reported.

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A novel series of [1,2,4]triazolo[4,3-a]quinoxaline derivatives of different heteroaromatization members were synthesized. The newly synthesized molecules were explored for their potential antimicrobial activities against a panel of pathogenic organisms. Among these derivatives, the chalcone compound 6e with a methoxy substituent exhibited broad potent antimicrobial activity against most of the bacterial and fungal strains.

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Novel flavanones that incorporate chromene motifs are synthesized via a one-step multicomponent reaction. The structures of the new chromenes are elucidated by using IR, H-NMR, C-NMR, H-H COSY, HSQC, HMBC, and elemental analysis. The new compounds are screened for their antimicrobial and cytotoxic activities.

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In our endeavors to develop novel and powerful agents with antiproliferative activities, a series of β-enamionitriles, linked to the 8-bromo-1H-benzo[f]chromene moieties (4a-m), was designed and synthesized under microwave irradiation conditions. The structures of the target compounds were established on the basis of their spectral data: IR, H NMR, C NMR, C NMR-DEPT/APT, F NMR and MS. Furthermore, the antiproliferative properties were evaluated against the human cancer cell lines MCF-7, HCT-116, and HepG-2 in comparison to the positive controls Vinblastine and Doxorubicin, employing the viability assay.

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A novel series of halogenated β-enaminonitriles (4a-m), linked 9-bromo-1H-benzo[f]-hromene moieties, were synthesized via microwave irradiation and were predestined for their cytotoxic activity versus three cancer cell lines, namely: MCF-7, HCT-116, and HepG-2. Several of the tested compounds showed high growth inhibitory activities versus the tumor cell lines. Particularly, compounds 4c, 4d, 4f, 4h, 4j, 4l, and 4m demonstrated superior antitumor activities against the aforementioned cell lines.

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This report presents the development of a novel and primary model of sulfonamide compounds encompassing a chromene azo motif with the intent of becoming applicable for drug candidates in the cases of drug-resistant pathogens. The novel molecules (7a-n) have been synthesized via a two-step reaction. First, 4-((2, 4-dihydroxyphenyl)diazenyl)benzenesulfonamide (3a-e) were obtained through the reaction of their corresponding diazotized 4-aminobenzenesulfonamides (1a-e) with resorcinol, followed by the heterocyclization of 3a-e with arylidenemalononitriles (6a-d).

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Novel β-enaminonitrile/ester compounds (4, 6) and an imidate of 4 (9) were utilized as key scaffolds for the synthesis of newly 2-substituted 4H-benzo[h]chromene (7, 8, 10, 11, 13, 14) and 7H-benzo[h]chromeno[2,3-d]pyrimidine derivatives (15-19). The spectral data confirmed the successful isolation of the desired compounds. The targeted compounds were assessed for their in vitro anticancer activity against mammary gland breast cancer cell line (MCF-7), human colon cancer (HCT-116), and liver cancer (HepG-2), while doxorubicin, vinblastine, and colchicine were utilized as standard references drugs.

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Novel fused chromenes (,⁻) and pyrimidines (⁻) were designed, synthesized, and evaluated for their mammary gland breast cancer (MCF-7), human colon cancer (HCT-116), and liver cancer (HepG-2) activities. The structural identity of the synthesized compounds was established according to their spectroscopic analysis, such as FT-IR, NMR, and mass spectroscopy. The preliminary results of the bioassay disclosed that some of the target compounds were proven to have a significant antiproliferative effect against the three cell lines, as compared to Doxorubicin, Vinblastine, and Colchicine, used as reference drugs.

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In our effort to develop novel and powerful agents with anti-proliferative activity, two new series of 1H-benzo[f]chromene derivatives, 4a-h and 6a-h, were synthesised using heterocyclocondensation methodologies under microwave irradiation condition. The structures of the target compounds were established on the basis of their spectral data, IR, H NMR,  C NMR,  C NMR-DEPT/APT, and MS data. The new compounds have been examined for their anti-proliferative activity against three cancer cell lines, MCF-7, HCT-116, and HepG-2.

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A new class of thermochromic polynorbornene with pendent spiropyran moieties has been synthesized. Functionalization of norbornene monomers with spirobenzopyran moieties has been achieved using Steglich esterification. These new monomeric materials were polymerized via Ring Opening Metathesis Polymerization (ROMP).

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The design of novel materials with significant biological properties is a main target in drug design research. Chromene compounds represent an interesting medicinal scaffold in drug replacement systems. This report illustrates a successful synthesis and characterization of two novel series of compounds using multi-component reactions.

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A series of novel 4-benzo[]chromenes , -, , ; 7-benzo[]chromeno[2,3-]pyrimidines -, , and 14-benzo[]chromeno[3,2-][1,2,4]triazolo[1,5-]pyrimidine derivatives -, was prepared. The structures of the synthesized compounds were characterized on the basis of their spectral data. Some of the target compounds were examined for their antiproliferative activity against three cell lines; breast carcinoma (MCF-7), human colon carcinoma (HCT-116) and hepatocellular carcinoma (HepG-2).

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A series of 1H-benzo[f]chromene-2-carbonitriles was synthesized and evaluated for their cytotoxic activities against MCF-7, HCT-116, and HepG-2 cancer cells. The SAR studies reported that the substitution in the phenyl ring at 1-position of 1H-benzo[f]chromene nucleus with the specific group, H atom, or methoxy group at 9-position increases the ability of the molecule against the different cell lines.

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Three new series of chromene molecules have been synthesized in order to explore their antimicrobial activity. The series encompass 2-substituted 14-(4-halophenyl)-12-methoxy-14-benzo[]chromeno[3,2-][1,2,4]-triazolo[1,5-]pyrimidines -, 9-benzylideneamino-7-(4-halo-phenyl)-5-methoxy-8-imino-7-benzo-[]chromeno[2,3-]pyrimidines - and 3-ethoxycarbonyl-14-(4-halophenyl)-12-methoxy-14-benzo-[]chromeno[3,2-][1,2,4]triazolo[1,5-]pyrimidine-2-one derivatives -. The structure of these novel compounds were confirmed using IR, ¹H- and C-NMR as well as MS spectroscopy.

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In continuation of our endeavor towards the design and development of potent and effective antimicrobial agents, three series of phthalimide derivatives ( and ) were synthesized, fully characterized and evaluated for their potential antibacterial, antifungal and antimycobacterial activities. These efforts led to the discovery of nine compounds , and (MIC range from 0.49 to 31.

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Ternary clusters Cu(9)In(10)S(9)(SEt)(21)(PPh(3))(3) and Cu(11)In(6)S(7)(S(t)Bu)(15) were isolated from the UV-photolysis products of precursors (PPh(3))(2)CuIn(SEt)(4) and (PPh(3))(2)CuIn(S(t)Bu)(4), respectively, and structurally characterized.

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