Convenient Synthesis of 2,2′- and 4,4′-Methylenebisphenols with Bulky Alkyl Substituents and Evaluation of Their Antioxidant Activity

The work is devoted to a convenient procedure of the synthesis of 2,2′- and 4,4′-methylenebisphenols with alkyl substituents in heterogeneous catalysis. This compounds were obtained with yields up to 87% by reflux of 2,4- or 2,6-dialkylphenols with HCHO in n-octane in the presence of KSF clay. We found that the antioxidant activity on DPPH test for two novel methylenebisphenols having isobornyl fragments was comparable with control drugs.     

Synthesis of 4(3H)-Quinazolinone Derivatives and Their in vitro Antitumor Activity

Classical antifolates containing L-glutamic acid moiety in molecule have shortcomings such as drug resistance which is originated from the defective cell transport by mutation, and toxicity to the host which is due to unnecessarily long retention inside normal cells.[1] One strategy to overcome these shortcomings is to design nonclassical lipophilic inhibitors of folate requiring enzymes by deleting or modifying L-glutamic acid component from the folate analogues.     

Synthesis and Antitumor Activity of4β-(1,2,3-Triazol-1-yl) podophyllotoxins

SemisyntheticanaloguesofthenaturallyoccurringpodophyllotoxinIhaverenewedinterestinrecentyearsasaresultofthedevelopmentofetoposide(VP-16)asanticancerdrug'-'.Inpreviousstudies'-",wefoundthatanumberof46-amino-oramidopodophyllotoxinswereasactiveormoreactivethanVP-16.Here,wereportthesynthesisandinvitroantitllmoractivityofthree40-(l,2,3-triazol-l-yi)podophyllotoxinswithstructuralfeaturesshowninformulae2-4.The40-(l,2,3-triazol-l-yi)podophyll2-4weresynthesizedasshowninScheme1.Amixtureofpodophylloto…     

Synthesis,Crystal Structure and Antitumor Activity of a Novel Zn(Ⅱ) Complex with 2-(Nicotinoyloxy)acetic Acid Ligand

A novel Zn(Ⅱ) complex, [ZnL_2(H_2O)_4]·H_2O(1, HL = 2-(nicotinoyloxy)acetic acid), was synthesized using Zn(OAc)_2·2H_2O and 2-(nicotinoyloxy)acetic acid as raw materials. Its structure has been elucidated by elemental analysis, IR and single-crystal X-ray diffraction. The structural analysis revealed that complex 1 crystallizes in triclinic, space group P1 and the Zn(Ⅱ) atom is six-coordinated with two N atoms from two different 2-(nicotinoyloxy)acetate anion ligands and four O atoms from coordinated water molecules. Complex 1 forms a 3D network structure by O–H···O hydrogen bonds. The antitumor activities of 2-(nicotinoyloxy)acetic acid ligand and its Zn(Ⅱ) complex were evaluated against human lung adenocarcinoma A549 cells, human hepatoma SMMC-7721 cells and human colon carcinoma Wi Dr cells.     

Synthesis and Antitumor Activity of New Derivatives of Podophyllotoxin

ＳｙｎｔｈｅｓｉｓａｎｄＡｎｔｉｔｕｍｏｒＡｃｔｉｖｉｔｙｏｆＮｅｗＤｅｒｉｖａｔｉｖｅｓｏｆＰｏｄｏｐｈｙｌｌｏｔｏｘｉｎＹａｎＧｕａｎｇＷＡＮＧ；ＪｉａｎＬｉｎＰＡＮａｎｄＹａｏＺｕＣＨＥＮ（ＤｅｐａｒｔｍｅｎｔｏｆＣｈｅｍｉｓｔｒｙ，Ｚｈｅｊｉ...     

Synthesis and Antitumor Activity of an Analog of Phthalascidin

Ecteinascidin 743 (Et-743) is an exceedingly potent antitumor agent isolated from the extracts of the marine tunicate Ecteinascidia turbinate1 that is currently undergoing phase Ⅱ/Ⅲ clinical trials in Europe and the United States2. As the result of its …     

Synthesis of 2-(Substituted Benzylideneamino)-4-(4′-hydroxyphenyl) Thiazoles and Their O-Glucosides

2-Amino-4-(4′-hydroxyphenyl) thiazole 1a was prepared from reaction between p-hydroxyacetophenone, thiourea, and iodine; compound 1a was treated with several (aryl/hetro aryl) aldehydes to form 2-(substituted benzylideneamino)-4-(4′-hydroxyphenyl) thiazoles 2a–j, which were glucosylated by using acetobromoglucose as a glucosyl donor to afford 2-(substituted benzylideneamino)-4-(2, 3, 4, 6-tetera-o-acetyl-4′-o-β-d-glucosidoxyphenyl) thiazoles 3a–j, which further on during deacetylation produced 2-(substituted benzylideneamino)-4-(4′-o-β-d-glucosidoxyphenyl) thiazoles 4a–j. These compounds were evaluated for biological activity, and their structure was confirmed by IR, NMR, mass spectra, elemental, and chemical analysis.

     

Synthesis,Characterization and Biological Activity of (Z)-1-[2-(Triphenylstannyl]Cyclopentanol and Their Phenylhalostannyl Derivativies

ＩｎｔｒｏｄｕｃｔｉｏｎＴｈｅｉｏｄｏｄｅｍｅｔａｌａｔｉｏｎ［１］ｏｆｔｈｅｐｒｏｄｕｃｔｓｏｆｔｈｅｒｅａｃｔｉｏｎｓｂｅｔｗｅｅｎｔｒｉｐｈｅｎｙｌｔｉｎｈｙｄｒｉｄｅａｎｄｅｔｈｙｎｙｌ（ｈｙｄｒｏｘｙ）ｓｔｅｒｏｉｄｓ［２，３］ｙｉｅｌｄｓ...     

Hypervalent Iodine Oxidation of 1-Trimethylsilyloxy, 1-(2′-Trimethylsilyloxyphenyl)Ethene. Synthesis of 3-Coumaranone and 2,2′-Dihydroxyacetophenone

The oxidation of 1-trimethylsilyloxy,1-(2′-trimethylsilyloxyphenyl)ethene (6) with iodosobenzene, boron trifluoride etherate and water affords two major products, namely, 3-coumaranone (9, 31%) and 2, 2′-dihydroxyaceto-phenone (10, 25%). Formation of 9 is explained by neighboring group participation by the adjacent hydroxyl group.     

Synthesis and Novel Properties of Alkyl Thiphosporamidate Derivatives of Nucleosides

Novel alkyl thiophosphoramidate derivatives of nucleosde analogues(5) have been prepared by phosphochloridothioate chemistry.O-Isopropyl 2‘,3‘-O-isopropylidene uridine-5‘-yl N-thiophosphoryl threonine and serine methyl esters(5a and 5b )underwent the intramolecular catalyzed hydrolysis reaction.     

Synthesis and Transformations of Substituted 3,3′-Diquinolinyl Sulfides

Abstract

Reactions of the 1,4-dithiin ring opening in 1,4-dithiinodiquinoline 1 with selected oxygen nucleophiles followed by S- and N-alkylation led to sulfides possessing one or two quinolinyl or quinolonyl units. Diquinolinyl sulfides 2 were transformed into quinolinyl-quinolonyl sulfides 3 or diquinolonyl sulfides 9 via thermal rearrangement (the O-N alkyl migration) or hydrolysis of the alkoxy and alkylthio groups with the hydrochloric acid-ethanol mixture.     

Crystal Structure and Antitumor Activity of Tri[2- [N-(4''''-methyl-benzylsulfonyl)amino]ethyl]-amine

1 INTRODUCTION The supramolecular architectures of tripodal ligands with special cavities have attracted much attention of chemists and biochemists because of their interesting structures and possible properties such as ion and molecular recognition, selective inclusion and important biological function[1～5]. However, their potential applications in supra- molecular and biological chemistry for constructing various complexes have not been clearly realized until recent years. Few crystal…     

Studies on Synthesis and Antitumor Activity of Phosphorylated Achyranthes bidentata Polysaccharide (P-AbPS)

ＩｎｔｒｏｄｕｃｔｉｏｎＩｔｉｓｗｅｌｌｋｎｏｗｎｔｈａｔｔｈｅｌｉｐｏｐｏｌｙｓａｃｃｈａｒｉｄｅｓａｒｅｃａ ｐａｂｌｅｏｆｒｅｖｅａｌｉｎｇａｖａｒｉｅｔｙｏｆｂｉｏｌｏｇｉｃａｌａｃｔｉｖｉｔｉｅｓｉｎｃｌｕｄ ｉｎｇｔｕｍｏｒ ｇｒｏｗｔｈｉｎｈｉｂｉｔｏｒｙａｃｔｉｖｉｔｙ .1Ｐｈｏｓｐｈｏｒｙｌａｔｉｏｎｏｆｐｏｌｙｓａｃｃｈａｒｉｄｅｓｈａｓａｔｔｒａｃｔｅｄｗｉｄｅｓｐｒｅａｄａｔｔｅｎｔｉｏｎｂｅｃａｕｓｅｉｔｗａｓｒｅｐｏｒｔｅｄｔｈａｔｔｈｅｙｓｈｏｗａｎｔｉｔｕｍｏｒａｃｔ…     

Crystal Structure and Antitumor Activity of Tri[2-[N-（4′-methyl-benzylsulfonyl）amino]ethyl]-amine

The crystal structure of the title compound (C27H38N4O7S3, Mr = 626.79) has been determined by single-crystal X-ray diffraction. The crystal is of triclinic, space group Pīwith a = 9.411(1), b = 11.645(2), c = 14.672(2) (A。), α = 91.80(1), β = 95.36(1), γ =104.56(1)o, V = 1547.0 (A。)3, Z = 2, Dc = 1.346 g/cm3, λ = 0.71073 (A。), μ(MoKα) = 0.289 mm－1 and F(000) = 664. The structure was refined to R = 0.0406 and wR = 0.1177 for 4103 observed reflections with I > 2σ(I). X-ray diffraction analysis reveals that the title compound is a practically distorted tetrahedron and each molecule contains one lattice H2O by hydrogen bond. The antitumor activity of the title compound against HL-60 human leukemia cells has also been studied by MTT method.     

Synthesis of N-Aryl-2-(1′,6′-dihydro-6′-pyridazinone-3′-carbonyl) Thiosemicarbazides and Their Related Heterocyclic Compounds

Introduction Somepyridazineshavebeenexaminedforac- tivityagainstsporozoanandflagellateparasitesand forantiamebicactivity[1]. 6-Aryl-4,5-dihydro-3(2H)-pyridazinonesex- hibitvariousbiologicalpropertiesincludingreduc- tionofbloodpressure,inhibitionofplateletaggre- gation,antiinflammation,andstrongplateletag- gregationinhibitingactioncoupledwithahypoten- siveaction.Italsopossessesweakpositiveinotrop- icactivityforthemanagementofcongestiveheart failure.Threepara-substitueddihydropyridazi- nonesare…     

Synthesis of (+) or (-)-2-(8′-Diphenylphosphino-1′-naphthyl)oxazoline Ligands and Their Application in Pd-Catalyzed Allylic Alkylation Reaction

ＩｎｔｒｏｄｕｃｔｉｏｎＷｉｔｈｔｈｅｆａｍｏｕｓＤＩＯＰｌｉｇａｎｄ ,ＫａｇａｎｉｎｔｒｏｄｕｃｅｄｔｈｅｉｍｐｏｒｔａｎｔｃｏｎｃｅｐｔｏｆＣ2 ｓｙｍｍｅｔｒｙｉｎｌｉｇａｎｄｄｅｓｉｇｎ .1Ｈｏｗｅｖｅｒ ,ｉｔｉｓｎｏｔａｌｗａｙｓｔｒｕｅｔｈａｔａＣ2 ｓｙｍｍｅｔｒｉｃｌｉｇａｎｄｓｈｏｕｌｄｎｅｃｅｓｓａｒｉｌｙｂｅｓｕｐｅｒｉｏｒｔｏａｎｏｎ ｓｙｍｍｅｔｒｉｃｃｏｕｎ ｔｅｒｐａｒｔ .Ｔｒａｎｓｉｔｉｏｎｍｅｔａｌ ｃａｔａｌｙｚｅｄａｌｌｙｌｉｃａｌｋｙｌａｔｉｏｎｖｉａｓｙｍｍｅ…     

Synthesis and Antitumor Activity of C-2／C-10 Modified Analogues of Docetaxel

Four 10-propionyl docetaxel analogues (lla-d) with 2α-amido substituents were prepared, and their antitumor activity against three solid tumor cell lines and their drug-resistant counterparts were determined.     

Synthesis and some transformations of 2-(2′-thienyl)benzothiazole

Condensation of ortho-aminothiophenol with 2-thenoyl chloride in 1-methyl-2-pyrrolidone was used to synthesize 2-(2′-thienyl)benzothiazole. Its reactions of electrophilic (nitration, bromination, oxymethylation, formylation, acylation) and radical (nitration, arylation) substitution were studied.     

Synthesis and Properties of N,N′-Disubstituted Ureas and Their Isosteric Analogs Containing Polycyclic Fragments: III. Synthesis and Properties ofN-[2-(Adamantan-1-yl)ethyl]-N′-R-ureas

Russian Journal of Organic Chemistry - Methods have been developed for the synthesis of N,N′-disubstituted ureas containing an adamantane fragment separated from the urea nitrogen atom by an...     

Synthesis of Novel 4β-(1, 2, 3-Triazol-1-yl) Podophyllotoxins as Potential Antitumor Drugs

The synthesis, characterization and in vitro antitumor activity of two novel podophyllotoxins, 4β-(5-methyl-1, 2, 3-triazol-1-y1)podophyllotoxin (5) and 4β-(5-phenyl-1, 2, 3-triazol-1-y1)podophyllotoxin (6), are described.