Nahed M. Fathy

REARRANGEMENT STUDIES ON 1-TETRALYLIDENECYANOTHIOACETAMIDE : A DIFFERENT NOVEL SYNTHETIC ROUTES TO STRONG FLUORESCENT PHENANTHRIDINE AND PHENANTHRENE ANALOGUES

Abstract A novel synthesis of strong fluorescent phenanthridine and phenanthrene analogues utilizing arylmethylenecyanothioacetamides and 1-tetralylidenemalononitrile or 1-tetralylidenecyanothioacetamide and arylmethylenemalononitriles as starting components is described.

Design, Synthesis and In vitro Anti-tumor Evaluation of Novel Acrylohydrazide Thioglycosides

A facile, convenient and high yielding synthesis of novel Acrylohydrazide thioglycosides via one-pot reaction of the potassium thiolate salts of aglycon part - prepared from readily available starting materials - with 2,3,4,6-tetra-O-acetyl- α-D-gluco- and galactopyranosyl bromides . Pharmacological evaluation of compounds 8j, 8b, 8h, 8k, 8f and 5b in vitro against (MCF-7) cell line (Breast carcinoma cell line) showing high- moderate anti-tumor activities with IC50 values ranging from 3.69-14.93 (μM), moreover molecular modeling of these compounds revealed that they have high binding affinity through hydrophobic-hydrophobic interaction and moderate selectivity through the hydrogen bond interaction with the atypical nucleotide binding pocket in the amino terminus of Hsp90.

Novel Synthesis of a New Class of Polynuclear Pyridinethione Nucleosides

Abstract A novel synthesis of a new class of polynuclear pyridinethione glycosides utilizing the reactions of phenanthridine analogues and α-bromoglucose or α-bromogalactose tetraacetate as starting components is described.

S-glycosides in medicinal chemistry: Novel synthesis of cyanoethylene thioglycosides and their pyrazole derivatives

ABSTRACT A one-pot reaction of a sodium 2-cyanoethylene-1-thiolate salt with 2,3,4,6-tetra-O-acetyl-α-D-gluco- and galactopyranosyl bromides affords a new class of cyanoethylene thioglycosides. The conversion to the corresponding 5-aminopyrazoles confirms the E-configuration of these cyanoethylene thioglycosides.

Novel Synthesis of a New Class of Strongly FluorescentPhenanthridine Analogues

A novel synthesis of strongly fluorescent phenanthridine and phenanthrene analogues as a possible new class of laser dyes utilizing the reactions of tetralin-1-ylidenecyanothioacetamide or tetralin-1-ylidenemalononitrile with β-(2-furyl)- and β-(2-thienyl)-acrylonitriles is reported.

Synthesis and anticancer activity of new [(Indolyl)pyrazolyl]-1,3,4-oxadiazole thioglycosides and acyclic nucleoside analogs

ABSTRACT New [(Indolyl)pyrazolyl]-1,3,4-oxadiazole compounds and their derived thioglycosides as well as the corresponding sugar hydrazones were synthesized. The acyclo C-nucleoside analogs of the oxadiazoline base system were also prepared by reaction of acid hydrazides with aldehydo sugars followed by one pot process encompassing acetylation and cyclization of the synthesized hydrazones. The anticancer activity of the newly synthesized compounds was studied against colorectal carcinoma (HCT116), breast adenocarcinoma (MCF7) and prostate cancer (PC3) human tumor cell lines and a number of compounds showed moderate to high activities.

Antimetabolites: Design, synthesis, and cytotoxic evaluation of novel dihydropyridine thioglycosides and pyridine thioglycosides

ABSTRACT A convenient synthesis of a novel series of dihydropyridine and pyridine thioglycosides was developed. The evaluation of anti-proliferative activity against HepG-2 cell lines (liver carcinoma cell lines) shows that most of the compounds have antitumor activity, especially 5b, 5f, 5j, 5n, 7b, 7f, 7j, 7n, 8b, 8f, and 8j. The results of molecular docking reveal that these compounds have high binding affinity by hydrogen bond formation with the binding pocket of thymidylate synthase dihydrofolate reductase (TS-DHFR).

Design, synthesis, molecular docking and anti-hepatocellular carcinoma evaluation of novel acyclic pyridine thioglycosides

ABSTRACT A novel series of acyclic pyridine thioglycosides has been synthesized. Evaluation of the anti proliferative activity of these compounds against HEPG-2 cell lines (liver carcinoma cell lines) shows that most of the compounds have high anti-tumor activities especially 6b, 6c, 7b and 7c. Furthermore, in the modeling study, these compounds showed that they have high binding affinity with thymidylate synthase dihydrofolate reductase (TS-DHFR).

trans-Tetra­aqua­bis{(E)-2-cyano-1-[(ethoxy­carbon­yl)methyl­sulfan­yl]-2-(1-naphthyl­amino­carbon­yl)ethene-1-thiol­ato}calcium(II) diethyl ether disolvate

In the title compound, [Ca(C18H15N2O3S2)(H2O)4]·2C4H10O, the Ca atom, which lies on an inversion centre, is coordinated octahedrally by four water molecules and two anions of the ketene dithioacetal, the donor atoms of which are the amidic carbonyl O atoms. The central backbone of the ligands (excluding the naphthalene and oxoethyl groups) is essentially planar (r.m.s. deviation 0.035 Å). Intramolecular hydrogen bonds are observed from the NH group to the formally ‘thiolate’ S atom and from one coordinated water to the nitrile group and to the ether O atom. Intermolecular hydrogen bonds from the second independent water molecule to the thiolate S atom and the side-chain oxo group connect the molecules in chains parallel to the a axis.