A. M. Soliman

Synthesis, antitumor activity and molecular docking study of novel sulfonamide-Schiff's bases, thiazolidinones, benzothiazinones and their C-nucleoside derivatives.

A series of sulfapyridine-polyhydroxyalkylidene (or arylidene)-imino derivatives (Schiffs bases) 2a-c and 4a-e were prepared by condensation of 4-amino-N-pyridin-2-ylbenzenesulfonamide (1) with different monosaccharides or with aromatic aldehydes. Treatment of 2a-c with thioglycolic acid led to the formation of the C-nucleosides (3a-c), while treatment of 4a-e with thioglycolic and/or thiosalicylic acids afforded the corresponding 2-arylthiazolidin-4-one or 2-arylbenzothiazin-4-one derivatives 5a-e and/or 6a-e, respectively. Some representative examples of the newly prepared compounds showed considerable cytotoxic effect against breast carcinoma cell line MCF7 and cervix carcinoma cell line HELA in comparison with 5-flurouracil and doxorubicin. AutoDock molecular docking into PTK has been done for lead optimization of the compounds in study as potential PTK inhibitors.

Dielectric relaxation study of alcohol/diol(s) mixtures

Abstract The dielectric relaxation of binary and ternary diol(s)/alcohol mixtures has been studied. Diols of different chain length namely 1,2 ethanediol, 1,3 propanediol, 1,4 butanediol and 1.5 pentanediol are used. The monohydric alcohols used are benzyl, n-hexyl, cyclopentyl, cyclohexyl and cycloheptyl alcohol. The relaxation spectra have been analyzed in one Cole-Davidson term. An apparent dipole moment term and the effective relaxation time of the main dispersion region are given as function of the number density of dipoles N D .

Synthesis and Antimicrobial Activity of Some Novel Quinoxalines

Abstract 2-Hydrazino-3-chloroquinoxaline 2 was prepared and reacted with active methylene compounds, potassium thiocyanate, carbon disulfide, phenylisothiocyanate, acetic acid, ethyl chloroformate, triethyl orthoformate, and Lawessens reagent (LR) to give a new class of fused quinoxalines 4–16, respectively. Also, 2,3-dihydrazinoquinoxaline 3 was prepared and reacted with carbon disulfide, phenyl isothiocyanate, and triethyl orthoformate to give the corresponding di[1,2,4] triazolo-[4,3-a:3′,4′-c]-quinoxalines 17–19, respectively. Reaction of 3 with LR gave the corresponding di[1,2,4,3]triazophospholo[4,5-a:5′,4′-c]quinoxaline-1,6-dithione (20). It was found that all synthesized compounds exhibit antimicrobial activity and that compound 20 had a broad spectrum of activity. GRAPHICAL ABSTRACT

A New Flavonoid from Limonium axillare

A new flavonol glycoside identified as myricetin 3‐O‐β‐D‐sor‐boside (1) has been isolated from the leaves of L. axillare. The new compound showed a moderate inhibition of Ehrlich ascites carci‐noma cells.

SYNTHESIS OF POLYFUSED HETEROCYCLIC SYSTEMS DERIVED FROM FUNCTIONALLY SUBSTITUTED THIENO(2,3-b)THIOPHENE MOEITY

Abstract Diethyl 3,4-diaminothieno(2,3-b)thiophene-2,5-dicarboxylate 1 was converted into the sodium salt of the corresponding acid 2. Compound 2 upon treatment with acetic anhydride furnished the bisoxazinone derivative 3. The reaction of compound 3 with ammonium acetate, hydrazine hydrate or aniline afforded the bispyrimidine derivatives 4, 5, or 6 respectively. The reaction of compound 4 with phosphoryl chloride gave the corresponding chloro derivative 7 which was converted into the corresponding hydrazino derivative 8. Treatment of compound 8 with acetylacetone or ethyl acetoacetate gave compounds 9 or 10, respectively. On the other hand, the reaction of compound 1 with hydrazine hydrate gave the corresponding hydrazide derivative 11 which was also treated with acetylacetone, ethyl acetoacetate, formic acid or acetic anhydride to afford the described compounds 12, 13, 14, or 15, respectively.

Synthesis of some new dispiro[dipyrano-(2,4′:6,4″)bidithiolo(4,5-b:4′,5′-e)-4,8-benzoquinones]

SummaryThe one pot reaction of acetylacetone, CS2, and tetrabromobenzoquinone in a 2:2:1 molar ratio affords 2,6-di-(1-acetyl-2-oxopropylidene)-bidithiolo-(4,5-b:4′5′-e)-4,8-benzoquinone (3) which was allowed to react with some active methylene reagents in a 1:2 molar ratio to give the dispiro derivatives5–11. The reaction is assumed to proceedvia a hydrolysis of the two acetyl groups in compound3 followed by a nucleophilic addition of the active methylene reagents at the two ethylenic bonds and subsequent cyclization.ZusammenfassungDie Eintopfreaktion von Acetylaceton, CS2 und Tetrabrombenzochinon in einem molaren Verhältnis von 2:2:1 liefert 2,6-Di-(1-acetyl-2-oxopropyliden)-bidithiolo-(4,5-b:4′,5′-e)-4,8-benzochinon (3), das anschließend mit aktivierten Methylenverbindungen im Verhältnis 1:2 zu den Dispiroverbindungen5–11 umgesetzt wurde. Die Reaktion verläuft offenbar über eine Hydrolyse der beiden Acetylgruppen in Verbindung3, gefolgt von einer nucleophilen Addition der aktiven Methylengruppen an die ethylenischen Doppelbindungen und anschließender Cyclisierung.

Dielectric relaxation study of diol mixtures

The dielectric relaxation of binary and ternary diol mixtures was studied. Diols of different chain lengths namely ethane-1,2-diol, propane-1,3-diol, butane-1,4-diol and pentane-1,5-diol were used. The relaxation spectra were analyzed in a single Cole–Davidson term. The effective dielectric relaxation time is shown to depend exponentially on the number density of dipoles or molecules. An empirical equation is suggested.

Synthesis of Some Novel Fused Azole Derivatives

Abstract A novel synthesis of pyrazolopyrimidine derivatives was reported wherein 5-amino-1-benzoyl-3-(methylthio)-1H-pyrazole-4-carbonitrile was treated with formic acid, formamide, thioacetamide, carbon disulfide, and phenylisocyanate and phenylisothiocyanate. GRAPHICAL ABSTRACT

Novel Synthesis of Condensed Pyridin-2(1H)-one and Pyrimidine Derivatives

The reaction of N-chloroacetyl derivatives 6-10 with morpholine yielded N-morpholin-1-yl acetyl derivatives 11-15 , which were subjected to Thorpe-Zieler cyclization with sodium tert -butoxide to produce the corresponding condensed pyridin-2(1H)-one derivatives 16-20 . Treatment of compounds 1 , 6-10 with either malononitrile or p -chlorobenzylidinemalononitrile in presence of triethylamine, afforded the corresponding pyrimidines 21-25 , 27 and pyridine derivative 26 respectively. Moreover compound 1 a was treated with ethyl isothiocyanoacetate to give the corresponding piprazine derivative 28 .

SYNTHESIS OF SOME NEW PYRROLO-(2,3-f)BENZOPYRROL-4,8-DIONE DERIVATIVES

Some new functionally substituted pyrrolobenzopyrrole derivatives were obtained starting with 3,6-diamino-2,5-dibromo-1,4-benzoquinone derivatives and active methylene reagents.