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ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was e... more ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
N-[(5-Cyano-2-oxoimidazolidin-4-yl)-iminomethyl]-p-toluensulfonamide 3 was prepared in fairly goo... more N-[(5-Cyano-2-oxoimidazolidin-4-yl)-iminomethyl]-p-toluensulfonamide 3 was prepared in fairly good yield by the base catalyzed cyclisation of N-[(Z)-2-amino-1,2-dicycanovinylcarbamoyl]-p-toluenesulfon-amide 2. The N-[(Z)-2-amino-1,2-dicycanovinyl carbamoyl]-p-toluenesulfonamide 2 was reacted readily with two molar amount of p-nitrobenzaldehyde at room temperature in the presence of base to give 7,8-dihy-dro-2-(4-nitrophenyl)-8-oxo-9-tosylpurine-6-carboxamide 8. Thiation of compounds 3 and 8 using Lawesson's reagent in tetrahydrofuran gave novel thioimidazoles 4, 5, and 6 and thiopurines 9, 10, and 11, which have been characterized spectroscopically.
The Stille coupling of tributylstannylthiophenes with halogenated tetrahydroisoquinolines produce... more The Stille coupling of tributylstannylthiophenes with halogenated tetrahydroisoquinolines produces analogues of michellamine alkaloids
3-(2-Chloroquinolin-3-yl)-1,5-bis(3,4,5-trimethoxy-phenyl)-pentane-2,4-dione derivatives 3a–b wer... more 3-(2-Chloroquinolin-3-yl)-1,5-bis(3,4,5-trimethoxy-phenyl)-pentane-2,4-dione derivatives 3a–b were conveniently synthesized in excellent yields (82% each) by tandem Knoevenagel condensation reactions of 2-chloro-3-carbaldehyde-quinoline 1a–b with 3,4,5-trimethoxy acetophenone, followed by a base catalyzed Michael addition, such as DBU (1,8-diazabicyclo[5,4,0]undec-7-ene) with or without solvent. The reactions of 3a–b with Pd(dba)2 in the presence of PPh3 (1:2) in degassed acetone provided the dinuclear palladium complexes {Pd(C,N-2-C9H4N–CH–[–CH2CO(3,4,5-(OMe-)3–C6H2-]2–3-R-6)Cl(PPh3)}2 [(R = H (4a), R = OMe (4b)] in moderate yields (38% and 43%), which in turn reacted with an excess of isonitrile XyNC (Xy = 2,6-Me2C6H3) to give the corresponding palladacycles 5a–b in moderate yields (45% and 43%). The palladacycles 5a–b were also obtained in similar yields (32% and 33%) via a one-pot oxidative addition reaction of 3a-b with isonitrile XyNC:Pd(dba)2 (4:1). The products were characterized by satisfactory elemental analysis and spectral studies (IR, 1H, and 31P NMR). The crystal structure of 5a was determined by X-ray crystallography diffraction studies.Novel palladacycles have been synthesized via a one-pot oxidative addition reaction of chloro-quinoline derivatives with Pd(dba)2 and 2,6-dimethylphenyl isocyanide XyNC (Xy = 2,6-Me2C6H3) or via the insertion reaction of isocyanide XyNC into a Pd–C bond of novel dinuclear palladium complexes. The sequence of reactions led eventually to compounds that could potentially possess pharmacological properties. The solid state structure of the selected complex 5a shows interesting features.
The quinolinylcyclopalladated complexes 3a–b were synthesised in good yields (81% and 77%) by the... more The quinolinylcyclopalladated complexes 3a–b were synthesised in good yields (81% and 77%) by the insertion reaction of the prepared dinuclear palladium complexes [Pd(C,N-2-C9H4N-CHO-3-R-6)Cl(PPh3)]2 [(R = H (2a), R = OMe (2b)] with isonitrile XyNC (Xy = 2,6-Me2C6H3). The cyclopalladated complexes 3a–b were also obtained in low yields (39% and 33.5%) via a one pot oxidative addition reaction of quinoline chloride 1a–b with isonitrile XyNC:Pd(dba)2 (4:1). The reactions of 3a–b with Tl(TfO) (TfO = triflate, CF3SO3) in the presence of H2O or EtOH causes depalladation reactions of the complexes to provide the corresponding organic compounds 4a–b, 5a–b and 6a–b in yields (41%, 27% and 18–19%). The products were characterized by satisfactory elemental analyses and spectral studies (IR, 1H, 13C and 31P NMR). The crystal structures of 2a, 3a and 3b were determined by X-ray diffraction studies.Some palladacycles have been synthesized from three simple and readily available building blocks via a one-pot oxidative addition reaction of quinoline chlorides to Pd(dba)2 and isocyanide XyNC or via the direct insertion reaction of XyNC into the prepared novel dinuclear palladium complexes. Depalladation reaction of the palladacycles could convert them into organic molecules. The sequence of reactions led eventually to compounds that could potentially possess pharmacological properties. The solid state structures of selected complexes 2a, 3a and 3b show interesting features.
Oxidative addition reactions of quinolines 1a, b with Pd(dba)2 in the presence of PPh3 (1 : 2) in... more Oxidative addition reactions of quinolines 1a, b with Pd(dba)2 in the presence of PPh3 (1 : 2) in acetone gave dinuclear palladium complexes [Pd(C,N-2-C9 H4N-CHO-3-R-6)Cl(PPh3)]2 [(R = H (2a), R = OMe (2b), which were reacted with isocyanide XyNC (Xy = ...
Dioncophielline and Michellamine Analogs S-5, R-5, S-7, R-7, S,S-8, R,R-8 and R,S-8 were synthesi... more Dioncophielline and Michellamine Analogs S-5, R-5, S-7, R-7, S,S-8, R,R-8 and R,S-8 were synthesized by using Stille coupling condition (Pd°-mediated cross coupling) proceeds in low yield when using stannanes 1 or 2 with tetrahydroisoquinolinyl bromide 3. The addition of tetrahydroisoquinolinyl iodide 4 instead of 3 significantly improves the efficiency of the coupling and providing a variety of Dioncophielline and Michellamine analogs in moderate yields.
... 5pKBH+ Values based on H,, are: a, -7.55; b, -7.22; c, -4.55; d, -4.43. 61t should be pointed... more ... 5pKBH+ Values based on H,, are: a, -7.55; b, -7.22; c, -4.55; d, -4.43. 61t should be pointed out that a slope s = 1 (as in Fig. lb ... Thiocarbonyls . [CrossRef] 2. Abdel-Sattar S. Hamad Elgazwy, Saad R. Atta-Allha, Sherif MAS Keshk. 2009. ...
A series of novel purine and pyrimidine derivatives were prepared and biologically evaluated for ... more A series of novel purine and pyrimidine derivatives were prepared and biologically evaluated for their in vitro anti-CDK2/cyclin A3 and antitumor activities in Ehrlich ascites carcinoma (EAC) cell based assay. The novel purine derivatives 13a,b demonstrated potent inhibitor activities with IC50 values of 14 ± 9 and 13 ± 9 μM, respectively. Additionally, compound 15a showed the highest potency (IC50 = 10 ± 6 μM) in EAC cell based assay. Molecular modeling study, including fitting to a 3D-pharmacophore model and their docking into cyclin dependant kinase2 (CDK2) active site showed high fit values and docking scores.The manuscript describes the investigation of a series of novel purine and pyrimidine derivatives, which were prepared in good yield by using diaminomaleonitrile and tosylisocyanate in acetonitrile. Molecular modeling studies, including fitting to a 3D-pharmacophore model their docking into cycline-dependent kinase2 (CDK2) active site were performed to understand the structural features of CDK2 inhibitors. Biological evaluation for both in vitro CDK2/cyclinA3 inhibition activity and antitumor activity in Ehrlich ascites carcinoma (EAC) cell based assay were also carried out.
Synthesis and Reactivity in Inorganic Metal-organic and Nano-metal Chemistry, 2009
The coordination behavior of nickel (II) chromium (III) and europium (III) with tricarballylic ac... more The coordination behavior of nickel (II) chromium (III) and europium (III) with tricarballylic acid (TCA) is described. Three new compounds Ni(II)-TCA, Cr(III)-TCA and Eu(III)-TCA were obtained and characterized of the species by elemental analysis, thermal behavior of TGA, DTA, ...
ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was e... more ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
N-[(5-Cyano-2-oxoimidazolidin-4-yl)-iminomethyl]-p-toluensulfonamide 3 was prepared in fairly goo... more N-[(5-Cyano-2-oxoimidazolidin-4-yl)-iminomethyl]-p-toluensulfonamide 3 was prepared in fairly good yield by the base catalyzed cyclisation of N-[(Z)-2-amino-1,2-dicycanovinylcarbamoyl]-p-toluenesulfon-amide 2. The N-[(Z)-2-amino-1,2-dicycanovinyl carbamoyl]-p-toluenesulfonamide 2 was reacted readily with two molar amount of p-nitrobenzaldehyde at room temperature in the presence of base to give 7,8-dihy-dro-2-(4-nitrophenyl)-8-oxo-9-tosylpurine-6-carboxamide 8. Thiation of compounds 3 and 8 using Lawesson's reagent in tetrahydrofuran gave novel thioimidazoles 4, 5, and 6 and thiopurines 9, 10, and 11, which have been characterized spectroscopically.
The Stille coupling of tributylstannylthiophenes with halogenated tetrahydroisoquinolines produce... more The Stille coupling of tributylstannylthiophenes with halogenated tetrahydroisoquinolines produces analogues of michellamine alkaloids
3-(2-Chloroquinolin-3-yl)-1,5-bis(3,4,5-trimethoxy-phenyl)-pentane-2,4-dione derivatives 3a–b wer... more 3-(2-Chloroquinolin-3-yl)-1,5-bis(3,4,5-trimethoxy-phenyl)-pentane-2,4-dione derivatives 3a–b were conveniently synthesized in excellent yields (82% each) by tandem Knoevenagel condensation reactions of 2-chloro-3-carbaldehyde-quinoline 1a–b with 3,4,5-trimethoxy acetophenone, followed by a base catalyzed Michael addition, such as DBU (1,8-diazabicyclo[5,4,0]undec-7-ene) with or without solvent. The reactions of 3a–b with Pd(dba)2 in the presence of PPh3 (1:2) in degassed acetone provided the dinuclear palladium complexes {Pd(C,N-2-C9H4N–CH–[–CH2CO(3,4,5-(OMe-)3–C6H2-]2–3-R-6)Cl(PPh3)}2 [(R = H (4a), R = OMe (4b)] in moderate yields (38% and 43%), which in turn reacted with an excess of isonitrile XyNC (Xy = 2,6-Me2C6H3) to give the corresponding palladacycles 5a–b in moderate yields (45% and 43%). The palladacycles 5a–b were also obtained in similar yields (32% and 33%) via a one-pot oxidative addition reaction of 3a-b with isonitrile XyNC:Pd(dba)2 (4:1). The products were characterized by satisfactory elemental analysis and spectral studies (IR, 1H, and 31P NMR). The crystal structure of 5a was determined by X-ray crystallography diffraction studies.Novel palladacycles have been synthesized via a one-pot oxidative addition reaction of chloro-quinoline derivatives with Pd(dba)2 and 2,6-dimethylphenyl isocyanide XyNC (Xy = 2,6-Me2C6H3) or via the insertion reaction of isocyanide XyNC into a Pd–C bond of novel dinuclear palladium complexes. The sequence of reactions led eventually to compounds that could potentially possess pharmacological properties. The solid state structure of the selected complex 5a shows interesting features.
The quinolinylcyclopalladated complexes 3a–b were synthesised in good yields (81% and 77%) by the... more The quinolinylcyclopalladated complexes 3a–b were synthesised in good yields (81% and 77%) by the insertion reaction of the prepared dinuclear palladium complexes [Pd(C,N-2-C9H4N-CHO-3-R-6)Cl(PPh3)]2 [(R = H (2a), R = OMe (2b)] with isonitrile XyNC (Xy = 2,6-Me2C6H3). The cyclopalladated complexes 3a–b were also obtained in low yields (39% and 33.5%) via a one pot oxidative addition reaction of quinoline chloride 1a–b with isonitrile XyNC:Pd(dba)2 (4:1). The reactions of 3a–b with Tl(TfO) (TfO = triflate, CF3SO3) in the presence of H2O or EtOH causes depalladation reactions of the complexes to provide the corresponding organic compounds 4a–b, 5a–b and 6a–b in yields (41%, 27% and 18–19%). The products were characterized by satisfactory elemental analyses and spectral studies (IR, 1H, 13C and 31P NMR). The crystal structures of 2a, 3a and 3b were determined by X-ray diffraction studies.Some palladacycles have been synthesized from three simple and readily available building blocks via a one-pot oxidative addition reaction of quinoline chlorides to Pd(dba)2 and isocyanide XyNC or via the direct insertion reaction of XyNC into the prepared novel dinuclear palladium complexes. Depalladation reaction of the palladacycles could convert them into organic molecules. The sequence of reactions led eventually to compounds that could potentially possess pharmacological properties. The solid state structures of selected complexes 2a, 3a and 3b show interesting features.
Oxidative addition reactions of quinolines 1a, b with Pd(dba)2 in the presence of PPh3 (1 : 2) in... more Oxidative addition reactions of quinolines 1a, b with Pd(dba)2 in the presence of PPh3 (1 : 2) in acetone gave dinuclear palladium complexes [Pd(C,N-2-C9 H4N-CHO-3-R-6)Cl(PPh3)]2 [(R = H (2a), R = OMe (2b), which were reacted with isocyanide XyNC (Xy = ...
Dioncophielline and Michellamine Analogs S-5, R-5, S-7, R-7, S,S-8, R,R-8 and R,S-8 were synthesi... more Dioncophielline and Michellamine Analogs S-5, R-5, S-7, R-7, S,S-8, R,R-8 and R,S-8 were synthesized by using Stille coupling condition (Pd°-mediated cross coupling) proceeds in low yield when using stannanes 1 or 2 with tetrahydroisoquinolinyl bromide 3. The addition of tetrahydroisoquinolinyl iodide 4 instead of 3 significantly improves the efficiency of the coupling and providing a variety of Dioncophielline and Michellamine analogs in moderate yields.
... 5pKBH+ Values based on H,, are: a, -7.55; b, -7.22; c, -4.55; d, -4.43. 61t should be pointed... more ... 5pKBH+ Values based on H,, are: a, -7.55; b, -7.22; c, -4.55; d, -4.43. 61t should be pointed out that a slope s = 1 (as in Fig. lb ... Thiocarbonyls . [CrossRef] 2. Abdel-Sattar S. Hamad Elgazwy, Saad R. Atta-Allha, Sherif MAS Keshk. 2009. ...
A series of novel purine and pyrimidine derivatives were prepared and biologically evaluated for ... more A series of novel purine and pyrimidine derivatives were prepared and biologically evaluated for their in vitro anti-CDK2/cyclin A3 and antitumor activities in Ehrlich ascites carcinoma (EAC) cell based assay. The novel purine derivatives 13a,b demonstrated potent inhibitor activities with IC50 values of 14 ± 9 and 13 ± 9 μM, respectively. Additionally, compound 15a showed the highest potency (IC50 = 10 ± 6 μM) in EAC cell based assay. Molecular modeling study, including fitting to a 3D-pharmacophore model and their docking into cyclin dependant kinase2 (CDK2) active site showed high fit values and docking scores.The manuscript describes the investigation of a series of novel purine and pyrimidine derivatives, which were prepared in good yield by using diaminomaleonitrile and tosylisocyanate in acetonitrile. Molecular modeling studies, including fitting to a 3D-pharmacophore model their docking into cycline-dependent kinase2 (CDK2) active site were performed to understand the structural features of CDK2 inhibitors. Biological evaluation for both in vitro CDK2/cyclinA3 inhibition activity and antitumor activity in Ehrlich ascites carcinoma (EAC) cell based assay were also carried out.
Synthesis and Reactivity in Inorganic Metal-organic and Nano-metal Chemistry, 2009
The coordination behavior of nickel (II) chromium (III) and europium (III) with tricarballylic ac... more The coordination behavior of nickel (II) chromium (III) and europium (III) with tricarballylic acid (TCA) is described. Three new compounds Ni(II)-TCA, Cr(III)-TCA and Eu(III)-TCA were obtained and characterized of the species by elemental analysis, thermal behavior of TGA, DTA, ...
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