The Experts below are selected from a list of 212943 Experts worldwide ranked by ideXlab platform
Feng Yang - One of the best experts on this subject based on the ideXlab platform.
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developing anticancer ferric prodrugs based on the n donor residues of human serum albumin carrier iia subdomain
Journal of Medicinal Chemistry, 2016Co-Authors: Yi Gou, Yao Zhang, Kun Yang, Shifang Chen, Li Liu, Tao Wang, Wei Zhang, Feng YangAbstract:To improve the selectivity, delivery, and activity of ferric (Fe) anticancer agents, we design prodrugs based on N-donor residues of the human serum albumin (HSA) carrier IIA subdomain. We synthesized six Fe(III) compounds derived from 2-hydroxy-1-naphthaldehyde thiosemicarbazone (7–12). HSA complex structure revealed that Fe compound binds to the hydrophobic cavity in the HSA IIA subdomain. Lys199 and His242 of HSA replace the two Cl atoms of Fe compound, coordinating with Fe3+. In vivo data revealed that compound 12 and HSA-12 complex inhibit the growth of the liver tumor and that the HSA-12 complex has stronger targeting ability and therapeutic efficacy than compound 12 alone. In addition, our results have shown that compound 12 and HSA-12 complex induce Bel-7402 cell death possible by several mechanisms.
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developing anticancer copper ii pro drugs based on the nature of cancer cells and the human serum albumin carrier iia subdomain
Molecular Pharmaceutics, 2015Co-Authors: Yi Gou, Yao Zhang, Feng Yang, Joshuapaul Ajayi, Zuping Zhou, Hong LiangAbstract:To synergistically enhance the selectivity and efficiency of anticancer copper drugs, we proposed and built a model to develop anticancer copper pro-drugs based on the nature of human serum albumin (HSA) IIA subdomain and cancer cells. Three copper(II) compounds of a 2-hydroxy-1-naphthaldehyde benzoyl hydrazone Schiff-base ligand in the presence pyridine, imidazole, or indazole ligands were synthesized (C1-C3). The structures of three HSA complexes revealed that the Cu compounds bind to the hydrophobic cavity in the HSA IIA subdomain. Among them, the pyridine and imidazole ligands of C1 and C2 are replaced by Lys199, and His242 directly coordinates with Cu(II). The indazole and Br ligands of C3 are replaced by Lys199 and His242, respectively. Compared with the Cu(II) compounds alone, the HSA complexes enhance cytotoxicity in MCF-7 cells approximately 3-5-fold, but do not raise cytotoxicity levels in normal cells in vitro through selectively accumulating in cancer cells to some extent. We find that the HSA complex has a stronger capacity for cell cycle arrest in the G2/M phase of MCF-7 by targeting cyclin-dependent kinase 1 (CDK1) and down-regulating the expression of CDK1 and cyclin B1. Moreover, the HSA complex promotes MCF-7 cell apoptosis possibly through the intrinsic reactive oxygen species (ROS) mediated mitochondrial pathway, accompanied by the regulation of Bcl-2 family proteins.
Yi Gou - One of the best experts on this subject based on the ideXlab platform.
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developing anticancer ferric prodrugs based on the n donor residues of human serum albumin carrier iia subdomain
Journal of Medicinal Chemistry, 2016Co-Authors: Yi Gou, Yao Zhang, Kun Yang, Shifang Chen, Li Liu, Tao Wang, Wei Zhang, Feng YangAbstract:To improve the selectivity, delivery, and activity of ferric (Fe) anticancer agents, we design prodrugs based on N-donor residues of the human serum albumin (HSA) carrier IIA subdomain. We synthesized six Fe(III) compounds derived from 2-hydroxy-1-naphthaldehyde thiosemicarbazone (7–12). HSA complex structure revealed that Fe compound binds to the hydrophobic cavity in the HSA IIA subdomain. Lys199 and His242 of HSA replace the two Cl atoms of Fe compound, coordinating with Fe3+. In vivo data revealed that compound 12 and HSA-12 complex inhibit the growth of the liver tumor and that the HSA-12 complex has stronger targeting ability and therapeutic efficacy than compound 12 alone. In addition, our results have shown that compound 12 and HSA-12 complex induce Bel-7402 cell death possible by several mechanisms.
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developing anticancer copper ii pro drugs based on the nature of cancer cells and the human serum albumin carrier iia subdomain
Molecular Pharmaceutics, 2015Co-Authors: Yi Gou, Yao Zhang, Feng Yang, Joshuapaul Ajayi, Zuping Zhou, Hong LiangAbstract:To synergistically enhance the selectivity and efficiency of anticancer copper drugs, we proposed and built a model to develop anticancer copper pro-drugs based on the nature of human serum albumin (HSA) IIA subdomain and cancer cells. Three copper(II) compounds of a 2-hydroxy-1-naphthaldehyde benzoyl hydrazone Schiff-base ligand in the presence pyridine, imidazole, or indazole ligands were synthesized (C1-C3). The structures of three HSA complexes revealed that the Cu compounds bind to the hydrophobic cavity in the HSA IIA subdomain. Among them, the pyridine and imidazole ligands of C1 and C2 are replaced by Lys199, and His242 directly coordinates with Cu(II). The indazole and Br ligands of C3 are replaced by Lys199 and His242, respectively. Compared with the Cu(II) compounds alone, the HSA complexes enhance cytotoxicity in MCF-7 cells approximately 3-5-fold, but do not raise cytotoxicity levels in normal cells in vitro through selectively accumulating in cancer cells to some extent. We find that the HSA complex has a stronger capacity for cell cycle arrest in the G2/M phase of MCF-7 by targeting cyclin-dependent kinase 1 (CDK1) and down-regulating the expression of CDK1 and cyclin B1. Moreover, the HSA complex promotes MCF-7 cell apoptosis possibly through the intrinsic reactive oxygen species (ROS) mediated mitochondrial pathway, accompanied by the regulation of Bcl-2 family proteins.
Karuppannan Natarajan - One of the best experts on this subject based on the ideXlab platform.
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x ray crystallographic investigation and biological activities of ru iii complexes containing schiff base and triphenyl phosphine arsine
Inorganica Chimica Acta, 2006Co-Authors: R Prabhakaran, R Huang, Karuppannan NatarajanAbstract:Abstract The crystal structures of the complexes [RuCl(Nap- o -phd)(AsPh 3 )] and [RuBr(Nap- o -phd)(PPh 3 )] (where H 2 -Nap- o -phd = N , N ′-bis(2-hydroxy-1-naphthaldehyde) o -phenylenediamine) have been determined by single crystal X-ray diffraction techniques. The antibacterial properties of the complexes have also been examined.
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spectral redox and catalytic studies of triphenylphosphine triphenylarsine complexes of ru iii with n o donor ligands derived from 2 hydroxy 1 naphthaldehyde and primary amines
Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy, 2006Co-Authors: V Mahalingam, Vaiapuri Chinnusamy, R Karvembu, Karuppannan NatarajanAbstract:Abstract A series of new mixed ligand hexacoordinated ruthenium(III) Schiff base complexes of the type [RuX 2 (EPh 3 ) 2 (LL′)] (X = Cl, E = P; X = Cl or Br, E = As and LL′ = anion of the Schiff bases derived from the condensation of 2-hydroxy-1-naphthaldehyde with aniline, 4-chloroaniline, 2-methyl aniline and 4-methoxy aniline) are reported. All the complexes have been characterized by analytical and spectral (IR, electronic and EPR) data. The redox behavior of the complexes has also been studied. The complexes exhibit catalytic activity in the oxidation of benzyl alcohol to benzaldehyde in the presence of N -methyl morpholine- N -oxide (NMO). An octahedral structure has been proposed for all of the complexes.
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preparation spectral characterization electrochemistry exafs antibacterial and catalytic activity of new ruthenium iii complexes containing ons donor ligands with triphenylphosphine arsine
Applied Organometallic Chemistry, 2006Co-Authors: R Prabhakaran, Venkata Krishnan, K Pasumpon, Duraiswamy Sukanya, Eric Wendel, Chinnasamy Jayabalakrishnan, Helmut Bertagnolli, Karuppannan NatarajanAbstract:New hexa-coordinated ruthenium (III) complexes of the type [RuX(EPh3)2(L)] (X = Cl or Br; L = dibasic tridentate Schiff base ligand; E = P or As) have been synthesized by the reactions of [RuCl3(PPh3)3], [RuCl3(AsPh3)3] or [RuBr3(AsPh3)3] with the appropriate Schiff base ligands derived by the condensation of salicylaldehyde and 2-hydroxy-1-naphthaldehyde with N(4) substituted thiosemicarbazones. All the new complexes were characterized using various physico-chemical methods such as elemental analyses, infrared, electron paramagnetic resonance (EPR) spectroscopy, magnetic moment and cyclic voltammetry. Based on the extended X-ray absorption fine structure (EXAFS) analysis, an octahedral structure has been confirmed for the complexes. The new complexes have been subjected to the catalytic activity and antibacterial studies. Copyright © 2005 John Wiley & Sons, Ltd.
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ruthenium ii complexes containing triphenylphosphine triphenylarsine and bidentate schiff bases derived from 2 hydroxy 1 naphthaldehyde and primary amines
Transition Metal Chemistry, 2004Co-Authors: K P Balasubramanian, Vaiapuri Chinnusamy, R Karvembu, Karuppannan NatarajanAbstract:The synthesis and characterisation of some new hexa-coordinated Schiff base complexes of the type [RuCl(CO)(EPh3)(B)(L)] (E = P or As; B = PPh3 or AsPh3 or py or pip; L = anion of the Schiff bases derived from 2-hydroxy-1-naphthaldehyde and aniline, 4-chloroaniline or 2-methylaniline) are reported. I.r., electronic, 1H-n.m.r, 31P-n.m.r. spectra, catalytic activity and antibacterial activity of the complexes are discussed. An octahedral structure has been tentatively proposed for all the complexes.
M. I. Choudhary - One of the best experts on this subject based on the ideXlab platform.
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tyrosinase inhibitory lignans from the methanol extract of the roots of vitex negundo linn and their structure activity relationship
Phytomedicine, 2006Co-Authors: Abdul Malik, Aqeel Ahmad, Mahmud Tareq Hassan Khan, Sher Bahadar Khan, M. I. ChoudharyAbstract:Abstract Phytochemical investigation of the methanol extract of Vitex negundo afforded eight lignans; negundin A 1 , negundin B 2 , 6-hydroxy-4-(4-hydroxy-3-methoxy)-3-hydroxymethyl-7-methoxy-3,4-dihydro-2-naphthaledehyde 3 , vitrofolal E 4 , (+)-lyoniresinol 5 , (+)-lyoniresinol-3 α - O - β - d -glucoside 6 , (+)-(−)-pinoresinol 7 , and (+)-diasyringaresinol 8 . The structures of these compounds were elucidated unambiguously by spectroscopic methods including 1D and 2D NMR analysis and also by comparing experimental data with literature data. The tyrosinase inhibitory potency of these compounds has been evaluated and attempts to justify their structure–activity relationships have been made in the present work. The compound 5 was found to be the most potent (IC 50 =3.21 μM) while other compounds demonstrated moderate to potent inhibitions. It was found that the substitution of functional group(s) at C-2 and C-3 positions and the presence of the –CH 2 OH group plays a vital role in the potency of the compounds. The compound 5 can act as a potential lead molecule to develop new drugs for the treatment of hyperpigmentation associated with the high production of melanocytes.
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tyrosinase inhibitory lignans from the methanol extract of the roots of vitex negundo linn and their structure activity relationship
Phytomedicine, 2006Co-Authors: Abdul Malik, Aqeel Ahmad, Mahmud Tareq Hassan Khan, Sher Bahadar Khan, M. I. ChoudharyAbstract:Phytochemical investigation of the methanol extract of Vitex negundo afforded eight lignans; negundin A 1, negundin B 2, 6-hydroxy-4-(4-hydroxy-3-methoxy)-3-hydroxymethyl-7-methoxy-3,4-dihydro-2-naphthaledehyde 3, vitrofolal E 4, (+)-lyoniresinol 5, (+)-lyoniresinol-3alpha-O-beta-d-glucoside 6, (+)-(-)-pinoresinol 7, and (+)-diasyringaresinol 8. The structures of these compounds were elucidated unambiguously by spectroscopic methods including 1D and 2D NMR analysis and also by comparing experimental data with literature data. The tyrosinase inhibitory potency of these compounds has been evaluated and attempts to justify their structure-activity relationships have been made in the present work. The compound 5 was found to be the most potent (IC(50)=3.21 microM) while other compounds demonstrated moderate to potent inhibitions. It was found that the substitution of functional group(s) at C-2 and C-3 positions and the presence of the -CH(2)OH group plays a vital role in the potency of the compounds. The compound 5 can act as a potential lead molecule to develop new drugs for the treatment of hyperpigmentation associated with the high production of melanocytes.
Laiwan Foong - One of the best experts on this subject based on the ideXlab platform.
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inner coordination sphere tin iv complexes with some o n n terdentate n 2 hydroxybenzaldehyde 1 amino 2 phenyleneimine and n 2 hydroxy 1 naphthaldehyde 1 amino 2 phenyleneimine and o n n o quadridentate n n bis 2 hydroxybenzaldehyde 1 2 phenylenediim
Polyhedron, 1997Co-Authors: Siangguan Teoh, Guan-yeow Yeap, Laiwan FoongAbstract:From the reactions of SnCl 4 with organotin(IV) chlorides (RSnCl 3 , R 2 SnCl 2 and R 3 SnCl, where R = Bu, Me and Ph) with N -(2-hydroxybenzaldehyde)-1-amino-2-phenyleneimine, N -(2-hydroxyl-1-naphthaldehyde)-1-amino-2-phenyleneimine, N , N ′-bis(2-hydroxybenzaldehyde)-1,2-phenylenediimine and N , N ′-bis(2-hydroxy-1-naphthaldehyde)-1,2-phenylenediimine a series of complexes have been synthesized and characterized, respectively, by microanalytical, IR, and 1 H NMR spectroscopic methods. The Ph 2 SnCl 2 reacted with N -(2-hydroxy-1-naphthaldehyde)-1-amino-2-phenyleneimine giving Ph 2 Sn(NAPPDI) [where NAPPDI = deprotonated N , N ′-bis(2-hydroxy-1-naphthaldehyde)-1,2-phenylenediimine], wherein the former Schiff base exhibit a facile intramolecular CN bond cleavage and intermolecular CN bond formation.
