Chinna Rajesh | University of Delhi (original) (raw)
Papers by Chinna Rajesh
Journal of Nanomedicine & Nanotechnology, Jan 2, 2015
Department of Chemistry, University of Delhi, Delhi-110 007, India <em>E-mail</em>: d... more Department of Chemistry, University of Delhi, Delhi-110 007, India <em>E-mail</em>: dsrawat@chemistry.du.ac.in Fax: 91-11-27667501 <em>Manuscript received 10 June 2013, accepted 13 June 2013</em> The synthesis of a cytotoxic natural ester sintenin (7a) and twenty eight of its analogues including. nitrogen-containing heterocyclic indole moiety (7b-7t), saturated (10a-10d) and unsaturated (10e-10h) amides were earned out by convenient route via one-pot Wittig reaction in aqueous medium with improved yield. A systematic structure activtiy relationship of sintenin ester was designed by chemically modified derivatives in order to get better cytotoxictty.
An entry from the Cambridge Structural Database, the world's repository for small molecule cr... more An entry from the Cambridge Structural Database, the world's repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.
Described herein are aminoqunoline and aminoacridine based hybrids, pharmaceutical compositions a... more Described herein are aminoqunoline and aminoacridine based hybrids, pharmaceutical compositions and medicaments that include such aminoquinoline and aminoacridine based hybrids, and methods of using such compounds for diagnosing and/or treating infections, neurodegerative diseases or disorderes, inflammation, inflammation associated diseases and disorders, diseases or disorders that are treatable with dopamine agonists such as the restless leg syndrome
ACS Sustainable Chemistry & Engineering, 2015
A nanocomposite consisting of reduced graphene oxide and zinc oxide nanoparticles (RGO/ZnO) with ... more A nanocomposite consisting of reduced graphene oxide and zinc oxide nanoparticles (RGO/ZnO) with unique structural features was developed as an efficient sustainable amphiphilic heterogeneous catalyst for the synthesis of various 3-substituted indoles in water. The catalyst was recycled six times without significant loss of the catalytic activity. The higher environmental compatibility and sustainability factors such as smaller E-factor and higher atom economy make the
RSC Adv., 2014
Tetrabutylammonium valinate [NBu4][Val] ionic liquid functionalized Fe3O4 NPs (VSF) was used as a... more Tetrabutylammonium valinate [NBu4][Val] ionic liquid functionalized Fe3O4 NPs (VSF) was used as an efficient “quasi-homogeneous” catalyst for multi-component synthesis of 1,4-dihydropyridines and 2-amino-4-(indol-3-yl)-4H-chromenes at room temperature.
Tetrahedron Letters, 2014
ABSTRACT A facile protocol, using ethylene glycol as a recyclable promoting medium for the three ... more ABSTRACT A facile protocol, using ethylene glycol as a recyclable promoting medium for the three component reaction of indoles, aldehydes, and amines to form 3-aminoalkylated indoles, is developed.
ACS Medicinal Chemistry Letters, 2012
A class of hybrid molecules consisting of 4aminoquinoline and pyrimidine were synthesized and tes... more A class of hybrid molecules consisting of 4aminoquinoline and pyrimidine were synthesized and tested for antimalarial activity against both chloroquine (CQ)-sensitive (D6) and chloroquine (CQ)-resistant (W2) strains of Plasmodium falciparum through an in vitro assay. Eleven hybrids showed better antimalarial activity against both CQ-sensitive and CQ-resistant strains of P. falciparum in comparison to standard drug CQ. Four molecules were more potent (7−8fold) than CQ in D6 strain, and eight molecules were found to be 5−25-fold more active against resistant strain (W2). Several compounds did not show any cytotoxicity up to a high concentration (60 μM), others exhibited mild toxicities, but the selective index for the antimalarial activity was very high for most of these hybrids. Two compounds selected for in vivo evaluation have shown excellent activity (po) in a mouse model of Plasmodium berghei without any apparent toxicity. The X-ray crystal structure of one of the compounds was also determined.
Diagnostics
The classification of pancreatic cyst fluids can provide a basis for the early detection of pancr... more The classification of pancreatic cyst fluids can provide a basis for the early detection of pancreatic cancer while eliminating unnecessary procedures. A candidate biomarker, gastricsin (pepsin C), was found to be present in potentially malignant mucinous pancreatic cyst fluids. A gastricsin activity assay using a magnetic bead-based platform has been developed using immobilized peptide substrates selective for gastricsin bearing a dimeric rhodamine dye. The unique dye structure allows quantitation of enzyme-cleaved product by both fluorescence and surface enhanced Raman spectroscopy (SERS). The performance of this assay was compared with ELISA assays of pepsinogen C and the standard of care, carcinoembryonic antigen (CEA), in the same clinical sample cohort. A retrospective cohort of mucinous (n = 40) and non-mucinous (n = 29) classes of pancreatic cyst fluid samples were analyzed using the new protease activity assay. For both assay detection modes, successful differentiation of m...
Advanced Synthesis & Catalysis, 2013
ACS Applied Bio Materials
Green Chemistry
Multi-metallic hybrid nanocatalysts consisting of a porous metal oxide host and metal satellite g... more Multi-metallic hybrid nanocatalysts consisting of a porous metal oxide host and metal satellite guests serve as a heterogeneous interface for multi-step transformations of divergent and energy-challenging substrates.
Asian Journal of Organic Chemistry
ACS Sustainable Chemistry & Engineering
New J. Chem.
C1-alkynylation of tetrahydroisoquinoline (THIQ) with wide substrate scope was achieved via A3 co... more C1-alkynylation of tetrahydroisoquinoline (THIQ) with wide substrate scope was achieved via A3 coupling strategy from the reaction among THIQ, aldehydes and alkynes using CuO@Fe2O3 as a nanocatalyst under green reaction conditions.
ACS Sustainable Chemistry & Engineering
Tetrahedron Letters, 2016
CuO/Fe 2 O 3 NPs were found to be robust, green and sustainable nanocatalysts for the synthesis o... more CuO/Fe 2 O 3 NPs were found to be robust, green and sustainable nanocatalysts for the synthesis of trisub-stituted propargylamines by the reaction of propiolic acid, secondary amines and aldehydes via decar-boxylative A3 coupling reaction under solvent free conditions. Further, we explored the wide applicability of the present methodology by replacing the more reactive aldehydes with less reactive ketones to afford the tetrasubstituted propargylamines via decarboxylative KA2 reaction. The present method showed several advantages such as usage of magnetically recoverable with six times recyclability of nanocatalyst, follows green chemistry principles including low E-factor and high atom economy for the A3 and KA2 reactions as well as high turnover numbers through easy catalyst recycling.
Journal of Nanomedicine & Nanotechnology, Jan 2, 2015
Department of Chemistry, University of Delhi, Delhi-110 007, India <em>E-mail</em>: d... more Department of Chemistry, University of Delhi, Delhi-110 007, India <em>E-mail</em>: dsrawat@chemistry.du.ac.in Fax: 91-11-27667501 <em>Manuscript received 10 June 2013, accepted 13 June 2013</em> The synthesis of a cytotoxic natural ester sintenin (7a) and twenty eight of its analogues including. nitrogen-containing heterocyclic indole moiety (7b-7t), saturated (10a-10d) and unsaturated (10e-10h) amides were earned out by convenient route via one-pot Wittig reaction in aqueous medium with improved yield. A systematic structure activtiy relationship of sintenin ester was designed by chemically modified derivatives in order to get better cytotoxictty.
An entry from the Cambridge Structural Database, the world's repository for small molecule cr... more An entry from the Cambridge Structural Database, the world's repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, cell parameters, space group, experimental conditions and quality measures.
Described herein are aminoqunoline and aminoacridine based hybrids, pharmaceutical compositions a... more Described herein are aminoqunoline and aminoacridine based hybrids, pharmaceutical compositions and medicaments that include such aminoquinoline and aminoacridine based hybrids, and methods of using such compounds for diagnosing and/or treating infections, neurodegerative diseases or disorderes, inflammation, inflammation associated diseases and disorders, diseases or disorders that are treatable with dopamine agonists such as the restless leg syndrome
ACS Sustainable Chemistry & Engineering, 2015
A nanocomposite consisting of reduced graphene oxide and zinc oxide nanoparticles (RGO/ZnO) with ... more A nanocomposite consisting of reduced graphene oxide and zinc oxide nanoparticles (RGO/ZnO) with unique structural features was developed as an efficient sustainable amphiphilic heterogeneous catalyst for the synthesis of various 3-substituted indoles in water. The catalyst was recycled six times without significant loss of the catalytic activity. The higher environmental compatibility and sustainability factors such as smaller E-factor and higher atom economy make the
RSC Adv., 2014
Tetrabutylammonium valinate [NBu4][Val] ionic liquid functionalized Fe3O4 NPs (VSF) was used as a... more Tetrabutylammonium valinate [NBu4][Val] ionic liquid functionalized Fe3O4 NPs (VSF) was used as an efficient “quasi-homogeneous” catalyst for multi-component synthesis of 1,4-dihydropyridines and 2-amino-4-(indol-3-yl)-4H-chromenes at room temperature.
Tetrahedron Letters, 2014
ABSTRACT A facile protocol, using ethylene glycol as a recyclable promoting medium for the three ... more ABSTRACT A facile protocol, using ethylene glycol as a recyclable promoting medium for the three component reaction of indoles, aldehydes, and amines to form 3-aminoalkylated indoles, is developed.
ACS Medicinal Chemistry Letters, 2012
A class of hybrid molecules consisting of 4aminoquinoline and pyrimidine were synthesized and tes... more A class of hybrid molecules consisting of 4aminoquinoline and pyrimidine were synthesized and tested for antimalarial activity against both chloroquine (CQ)-sensitive (D6) and chloroquine (CQ)-resistant (W2) strains of Plasmodium falciparum through an in vitro assay. Eleven hybrids showed better antimalarial activity against both CQ-sensitive and CQ-resistant strains of P. falciparum in comparison to standard drug CQ. Four molecules were more potent (7−8fold) than CQ in D6 strain, and eight molecules were found to be 5−25-fold more active against resistant strain (W2). Several compounds did not show any cytotoxicity up to a high concentration (60 μM), others exhibited mild toxicities, but the selective index for the antimalarial activity was very high for most of these hybrids. Two compounds selected for in vivo evaluation have shown excellent activity (po) in a mouse model of Plasmodium berghei without any apparent toxicity. The X-ray crystal structure of one of the compounds was also determined.
Diagnostics
The classification of pancreatic cyst fluids can provide a basis for the early detection of pancr... more The classification of pancreatic cyst fluids can provide a basis for the early detection of pancreatic cancer while eliminating unnecessary procedures. A candidate biomarker, gastricsin (pepsin C), was found to be present in potentially malignant mucinous pancreatic cyst fluids. A gastricsin activity assay using a magnetic bead-based platform has been developed using immobilized peptide substrates selective for gastricsin bearing a dimeric rhodamine dye. The unique dye structure allows quantitation of enzyme-cleaved product by both fluorescence and surface enhanced Raman spectroscopy (SERS). The performance of this assay was compared with ELISA assays of pepsinogen C and the standard of care, carcinoembryonic antigen (CEA), in the same clinical sample cohort. A retrospective cohort of mucinous (n = 40) and non-mucinous (n = 29) classes of pancreatic cyst fluid samples were analyzed using the new protease activity assay. For both assay detection modes, successful differentiation of m...
Advanced Synthesis & Catalysis, 2013
ACS Applied Bio Materials
Green Chemistry
Multi-metallic hybrid nanocatalysts consisting of a porous metal oxide host and metal satellite g... more Multi-metallic hybrid nanocatalysts consisting of a porous metal oxide host and metal satellite guests serve as a heterogeneous interface for multi-step transformations of divergent and energy-challenging substrates.
Asian Journal of Organic Chemistry
ACS Sustainable Chemistry & Engineering
New J. Chem.
C1-alkynylation of tetrahydroisoquinoline (THIQ) with wide substrate scope was achieved via A3 co... more C1-alkynylation of tetrahydroisoquinoline (THIQ) with wide substrate scope was achieved via A3 coupling strategy from the reaction among THIQ, aldehydes and alkynes using CuO@Fe2O3 as a nanocatalyst under green reaction conditions.
ACS Sustainable Chemistry & Engineering
Tetrahedron Letters, 2016
CuO/Fe 2 O 3 NPs were found to be robust, green and sustainable nanocatalysts for the synthesis o... more CuO/Fe 2 O 3 NPs were found to be robust, green and sustainable nanocatalysts for the synthesis of trisub-stituted propargylamines by the reaction of propiolic acid, secondary amines and aldehydes via decar-boxylative A3 coupling reaction under solvent free conditions. Further, we explored the wide applicability of the present methodology by replacing the more reactive aldehydes with less reactive ketones to afford the tetrasubstituted propargylamines via decarboxylative KA2 reaction. The present method showed several advantages such as usage of magnetically recoverable with six times recyclability of nanocatalyst, follows green chemistry principles including low E-factor and high atom economy for the A3 and KA2 reactions as well as high turnover numbers through easy catalyst recycling.