Anti-hepatocellular carcinoma activities of novel hydrazone derivatives downregulation of interleukin-6.

Hepatocellular carcinoma (HCC) is one of the leading causes of cancer-related morbidity worldwide. Sorafenib is a first-line drug for the treatment of HCC, however, it is reported to cause serious adverse effects and may lead to resistance in many patients. In this study, 20 hydrazone derivatives incorporating triazoles, pyrazolone, pyrrole, pyrrolidine, imidazoline, quinazoline, and oxadiazine moieties were designed, synthesized, and characterized.

Design and synthesis of novel multi-target tetrabromophthalimides as CBS and Topo-II inhibitors and DNA intercalators.

Microtubules are highly dynamic structures and constitute a crucial component of the cellular cytoskeleton. Besides, topoisomerases (Topo) play a fundamental role in maintaining the appropriate structure and organization of DNA. On the other hand, dual mechanism drug candidates for cancer treatment primarily aim to enhance the efficacy of cancer treatment and potentially overcome drug resistance.

Design and synthesis of novel tetrabromophthalimide derivatives as potential tubulin inhibitors endowed with apoptotic induction for cancer treatment.

Although various approaches exist for treating cancer, chemotherapy continues to hold a prominent role in the management of this disease. Besides, microtubules serve as a vital component of the cellular skeleton, playing a pivotal role in the process of cell division making it an attractive target for cancer treatment. Hence, the scope of this work was adapted to design and synthesize new anti-tubulin tetrabromophthalimide hybrids (3-17) with colchicine binding site (CBS) inhibitory potential.

Biological evaluation, docking studies, and ADME prediction of some pyrimidine and pyridine derivatives as potential EGFR and EGFR inhibitors.

Herein, a set of pyridine and pyrimidine derivatives were assessed for their impact on the cell cycle and apoptosis. Human breast cancer (MCF7), hepatocellular carcinoma (HEPG2), larynx cancer (HEP2), lung cancer (H460), colon cancers (HCT116 and Caco2), and hypopharyngeal cancer (FADU), and normal Vero cell lines were used. Compounds and displayed outstanding effects on the investigated cell lines and were further tested for their antioxidant activity in MCF7, H460, FADU, HEP2, HEPG2, HCT116, Caco2, and Vero cells by measuring superoxide dismutase (SOD), malondialdehyde content (MDA), reduced glutathione (GSH), and nitric oxide (NO) content.

Design and synthesis of novel benzoazoninone derivatives as potential CBSIs and apoptotic inducers: In Vitro, in Vivo, molecular docking, molecular dynamics, and SAR studies.

Apparently, tubulin inhibitors binding to the colchicine-binding site (CBS) currently have outstanding attention for cancer treatment. So, a series of benzo[b]azonin-2-one derivatives having the same pharmacophoric features as colchicine binding site inhibitors (CBSIs) were synthesized targeting the CBS of β-tubulin. The antiproliferative activities of the newly synthesized compounds were assessed against five different cancer cell lines; HepG-2, MCF-7, MDA-MB-231, HCT-116, and Caco-2.

Synthesis, structural characterization, DFT calculations, molecular docking, and molecular dynamics simulations of a novel ferrocene derivative to unravel its potential antitumor activity.

In this article, we describe a set of subsequent five-steps chemical reactions to synthesize a ferrocene derivative named 1-(5-(diphenylphosphaneyl)cyclopenta-1,3-dien-1-yl)ethyl)imino)-1,3-dihydroisobenzofuran-5-yl)methanol (). Structural characterization of and its intermediate products was also performed and reported to attest to their formation. A molecular docking study was performed to propose the novel synthesized ferrocene derivative () as a potential antitumor candidate targeting the mitogen-activated protein (MAP) kinases interacting kinase (Mnk) 1.

Synthesis and in vitro Anticancer Activity of Novel Heterocycles Utilizing Thiophene Incorporated Thioureido Substituent as Precursors.

Ethyl 2-(3-allylthioureido)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylate (1) was used as a building block for synthesis of new heterocycles. Pyrimidine and thiazole moieties were achieved upon condensation of compound 1 with various reagents such as chloroacetic acid, dietyl malonate, ninhydrin, 2,3-epoxy-2,3-dihydro-1,4-naphthoquinone, and hydrazine hydrate. The structures of the newly synthesized compounds were confirmed using spectral measurements.

Synthesis of novel cyanine dyes as antitumor agents.

In this study, some novel cyanine dyes, 1, 3, and 5-15, were synthesized by a one-pot step reaction of pyridinium salts 2 and/or 4 with benzenaminium salt 1. N-{[1-Chloro-3,4-dihydronaphthalen-2-yl)methylene]benzenaminium} chloride 1 was obtained by the reaction of α-tetralone with Vilsmeier-Haack reagent, followed by a mixture of an equimolar ratio of anilin/ethanol (1:1). All new cyanine dyes were evaluated in vitro for their anticancer activity against two cell lines, that is, HepG2 (human hepatocellular liver carcinoma) and MCF-7 (breast cancer).

Zinc Oxide Nanoparticle Synergizes Sorafenib Anticancer Efficacy with Minimizing Its Cytotoxicity.

Cancer, as a group, represents the most important cause of death worldwide. Unfortunately, the available therapeutic approaches of cancer including surgery, chemotherapy, radiotherapy, and immunotherapy are unsatisfactory and represent a great challenge as many patients have cancer recurrence and severe side effects. Methotrexate (MTX) is a well-established (antineoplastic or cytotoxic) chemotherapy and immunosuppressant drug used to treat different types of cancer, but its usage requires high doses causing severe side effects.

Antimicrobial evaluation and docking study of some new substituted benzimidazole-2yl derivatives.

Benzimidazoles incorporated biologically active heterocycles such as quinoline, triazine-3-thione, thiazole and thiadiazole, were synthesized utilizing 2-acetylbenzimidazole as a building block. The structures of the newly synthesized benzimidazoles were assured by their spectral data (IR, H NMR, C- NMR and MS spectra). Most of the synthesized candidates were screened for their in vitro antimicrobial activity against Staphylococcus aureus, Escherichia coli, Bacillus pumilus and antifungal activity against (Saccharomyces cerevisiae).

Synthesis, Characterization, and Biochemical Impacts of Some New Bioactive Sulfonamide Thiazole Derivatives as Potential Insecticidal Agents against the Cotton Leafworm, .

A novel series of anticipated biologically active heterocyclic compounds, such as pyrazole, thiazole, pyridine, acrylamide, thiophene, triazolo[1,5-]pyrimidine, imidazolidine, aminopyrazole, pyrazolo[5,1-][1,2,4]triazine, triazolo[4,3-]pyrimidine, benzo[4,5]imidazo[1,2-]pyrimidine, pyrido[2',3':3,4]pyrazolo[5,1-][1,2,4]triazine, isoxazole, benzo[4,5]imidazo[2,1-][1,2,4]triazine, pyrimidine, pyrido[2',3':3,4]pyrazolo[1,5-]pyrimidine, pyrano[2,3-]pyrimidine, and chromene derivatives, incorporating a sulfonamide-bearing thiazole moiety suitable to utilize as insecticidal agents were synthesized via a versatile, readily accessible cyanoacetanilide, 2-cyano--(4-(-(thiazol-2-yl)sulfamoyl)phenyl)acetamide ().The structures of the newly synthesized compounds were elucidated by IR, MS, H NMR, C NMR, distortionless enhancement by polarization transfer (DEPT), H-H correlation spectroscopy (COSY), heteronuclear multiple bond correlation (HMBC), and heteronuclear single quantum coherence (HSQC) spectral analysis. Toxicological and biochemical parameters and biological aspects of the demonstrated compounds of the synthesized products against the cotton leafworm, , under laboratory conditions were also investigated.

Synthesis, molecular docking and antimicrobial activity of new fused pyrimidine and pyridine derivatives.

Synthesis of some new heterocyclic ring systems incorporated pyrimidine and pyridine moieties starting from 1-(furan-2-yl)-3-(thiophen-2-yl) chalcone was achieved. The structure of the new compounds was interpreted by spectral studies and ESI-MS analysis. Antimicrobial investigations of the designated compounds were performed towards some harmful pathogenic microbes.

Long term results of fixed-hinge megaprostheses in limb salvage for malignancy.

We retrospectively studied the files of 669 patients with musculoskeletal tumors treated with limb salvage and reconstruction using fixed-hinge knee megaprostheses. We used the KMFTR® prosthesis from 1983 to 1989 in 126 patients, and the HMRS® prosthesis thereafter in 543 patients because of the anatomical femoral stem with one lateral flange for improved stress-shielding, the new hinge design and new generation polyethylene placed centrally in the metallic hinge, and the improved function compared to the former prosthesis. Distal femoral reconstructions were done in 474, proximal tibia in 163, extrarticular knee joint in nine, and total femoral in 23 patients.

Soft-tissue recurrence of giant cell tumor of bone associated with pulmonary metastases.

A soft tissue recurrence associated with pulmonary metastases developed in a 46 year old lady one year after intra-lesional excision and autogenous bone graft of giant cell tumor of bone of the distal end of the right radius. The different imaging modalities and procedures used for staging as well as the management were discussed. Brief review of relevant literatures addressed different factors that influence addressed different factors that influence recurrence, treatment Options of primary and recurrent GCT of distal radius, and metaplastic recurrent GCT of distal radius, and metaplastic bone formation in such lesions.

Malignant bone tumors in Kuwait: a 10-year clinicopathological study.

Between 1995 and 2004, 142 malignant bone tumours comprising 76 primary and 66 secondary tumours were identified in the Pathology Department of Al-Sabah Hospital, Kuwait. Pathological fracture was the presenting sign in 35% of the cases. The mean incidence of primary tumours/year was 3.

Growth arrest resulting from unicameral bone cyst.

Growth arrest complicating unicameral bone cyst of the proximal humerus is reported in five patients. These patients represented 10% of 51 consecutive patients treated by the senior author at our hospital from 1988 through 1995. The youngest patient at first clinical presentation was aged 6 years, and the oldest was 14 years 9 months.