01206nas a2200217   4500008004100000022001400041245014600055210006900201260010600270300001400376490000700390520030900397653001400706653001800720653002900738653001900767653002200786100002800808700002200836856013000858       2006                        eng d  a0040-403900aCu(OTf)(2) or Et3N-catalyzed three-component condensation of aldehydes, amines and cyanides: a high yielding synthesis of alpha-aminonitriles0 aCuOTf2 or Et3Ncatalyzed threecomponent condensation of aldehydes  aTHE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLANDbPERGAMON-ELSEVIER SCIENCE LTDcAUG  a5759-57620 v473 a<p>Copper(II) triflate or Et3N have been found to catalyze, under ambient conditions, the addition of a cyanide anion, such as trimethylsilyl cyanide or acetone cyanohydrin, onto in situ generated imines, furnishing alpha-aminonitriles in excellent yields. (c) 2006 Elsevier Ltd. All rights reserved.</p>10aaldehydes10aaminonitriles10amulticomponent reactions10aorganocatalyst10aStrecker reaction1 aParaskar, Abhimanyu, S.1 aSudalai, Arumugam  uhttps://library.ncl.res.in/content/cuotf2-or-et3n-catalyzed-three-component-condensation-aldehydes-amines-and-cyanides-high-001389nas a2200229   4500008004100000022001400041245017700055210006900232260010600301300001400407490000700421520044300428653002300871653002500894653001600919653002100935653001400956653001500970100002800985700002201013856012401035       2006                        eng d  a0040-402000aEnantioselective synthesis of (-)-cytoxazone and (+)-epi-cytoxazone, novel cytokine modulators via sharpless asymmetric epoxidation and L-proline catalyzed mannich reaction0 aEnantioselective synthesis of cytoxazone and epicytoxazone novel  aTHE BOULEVARD, LANGFORD LANE, KIDLINGTON, OXFORD OX5 1GB, ENGLANDbPERGAMON-ELSEVIER SCIENCE LTDcJUN  a5756-57620 v623 a<p>A short and efficient enantioselective synthesis of (-)-cytoxazone and its stereoisomer (+)-epi-cytoxazone, novel cytokine modulators, has been described with good yield and enantioselectivity. Ti-catalyzed Sharpless asymmetric epoxidation of allyl alcohol and L-proline catalyzed three-component Mannich reaction constitute the key steps in introducing stereogenicity into the molecule. (c) 2006 Elsevier Ltd. All rights reserved.</p>10aaminohydroxylation10aAsymmetric synthesis10aepoxidation10aMannich reaction10aOxidation10aOzonolysis1 aParaskar, Abhimanyu, S.1 aSudalai, Arumugam  uhttps://library.ncl.res.in/content/enantioselective-synthesis-cytoxazone-and-epi-cytoxazone-novel-cytokine-modulators-001095nas a2200229   4500008004100000022001400041245007900055210006900134260008900203300001200292490000700304520024300311653002300554653002700577653002900604653002800633653001500661653003300676100002800709700002200737856010600759       2007                        eng d  a0376-469900aCu(OTf)(2) catalyzed high yield synthesis of hantzsch 1,4-dihydropyridines0 aCuOTf2 catalyzed high yield synthesis of hantzsch 14dihydropyrid  aDR K S KRISHNAN MARG, NEW DELHI 110 012, INDIAbNATL INST SCIENCE COMMUNICATIONcFEB  a331-3350 v463 a<p>Copper(II) triflate catalyzes efficiently the three-component condensation of aldehydes, beta-ketoesters and ammonium acetate in acetonitrile at 25 degrees C to afford the corresponding Hantzsch 1,4-dihydropyridines in high yields.</p>10a4-dihydropyridines10aanti-hypertensive drug10acalcium channel blockers10acardiovascular diseases10aHantzsch 110athree-component condensation1 aParaskar, Abhimanyu, S.1 aSudalai, Arumugam  uhttps://library.ncl.res.in/content/cuotf2-catalyzed-high-yield-synthesis-hantzsch-14-dihydropyridines01180nas a2200217   4500008004100000022001400041245014300055210006900198260010300267300001400370490000700384520030400391653001400695653001400709653001100723653002800734100002200762700002800784700002200812856012800834       2008                        eng d  a0376-469900aCu(OTf)(2) catalyzed Biginelli type condensation of aldehydes, beta-keto esters and carbamates: synthesis of 3,4-dihydro[1,3]oxazin-2-ones0 aCuOTf2 catalyzed Biginelli type condensation of aldehydes betake  aANUSANDHAN BHAWAN, 2 RAFI MARG, NEW DELHI, 110001, INDIAbCOUNCIL SCIENTIFIC & INDUSTRIAL REScJUL  a1091-10950 v473 a<p>Cu(OTf)(2) catalyzes effectively a new multicomponent reaction comprising aldehydes, beta-ketoester and methy carbamate in acetonitrile to afford substituted 3,4-dihydro[1,3]oxazin-2-ones in 60-82% yields. These compounds have been found to show inhibition activity against HL-60 cancer cell.</p>10aaldehydes10aCatalysts10aCopper10aMulticomponent reaction1 aJagdale, Arun, R.1 aParaskar, Abhimanyu, S.1 aSudalai, Arumugam  uhttps://library.ncl.res.in/content/cuotf2-catalyzed-biginelli-type-condensation-aldehydes-beta-keto-esters-and-carbamates-001309nas a2200217   4500008004100000022001400041245014200055210006900197260007500266300001200341520047000353653001300823653001100836653001400847653001100861653001500872100002200887700002800909700002200937856013200959       2009                        eng d  a0039-788100aCobalt(II) chloride hexahydrate-diisopropylamine catalyzed mild and chemoselective reduction of carboxylic esters with sodium borohydride0 aCobaltII chloride hexahydratediisopropylamine catalyzed mild and  aRUDIGERSTR 14, D-70469 STUTTGART, GERMANYbGEORG THIEME VERLAG KGcFEB  a660-6643 a<p>The cobalt-catalyzed reduction of unsaturated alpha-cyano carboxylic esters using sodium borohydride (NaBH(4)) leads to the corresponding saturated cyano alcohols in high yields. In particular, the new catalytic system cobalt(II) chloride-diisopropylamine in combination with NaBH(4) showed excellent activity in the chemoselective reduction of a variety of carboxylic esters to their corresponding alcohols in good to excellent yields under mild conditions.</p>10aAlcohols10aamines10acatalysis10aEsters10areductions1 aJagdale, Arun, R.1 aParaskar, Abhimanyu, S.1 aSudalai, Arumugam  uhttps://library.ncl.res.in/content/cobaltii-chloride-hexahydrate-diisopropylamine-catalyzed-mild-and-chemoselective-reduction-002646nas a2200313   4500008004100000022001400041245011600055210006900171260008000240300001600320490000800336520152500344653001101869653001701880653001701897100002801914700001801942700002201960700002601982700002402008700002102032700002802053700002202081700002002103700002702123700003202150700002502182856012502207       2010                        eng d  a0027-842400aHarnessing structure-activity relationship to engineer a cisplatin nanoparticle for enhanced antitumor efficacy0 aHarnessing structureactivity relationship to engineer a cisplati  a2101 CONSTITUTION AVE NW, WASHINGTON, DC 20418 USAbNATL ACAD SCIENCEScJUL  a12435-124400 v1073 a<p>Cisplatin is a first line chemotherapy for most types of cancer. However, its use is dose-limited due to severe nephrotoxicity. Here we report the rational engineering of a novel nanoplatinate inspired by the mechanisms underlying cisplatin bioactivation. We engineered a novel polymer, glucosamine-functionalized polyisobutylene-maleic acid, where platinum (Pt) can be complexed to the monomeric units using a monocarboxylato and an O –&gt; Pt coordinate bond. We show that at a unique platinum to polymer ratio, this complex self-assembles into a nanoparticle, which releases cisplatin in a pH-dependent manner. The nanoparticles are rapidly internalized into the endolysosomal compartment of cancer cells, and exhibit an IC50 (4.25 + 0.16 mu M) comparable to that of free cisplatin (3.87 +/- 0.37 mu M), and superior to carboplatin (14.75 +/- 0.38 mu M). The nanoparticles exhibited significantly improved antitumor efficacy in terms of tumor growth delay in breast and lung cancers and tumor regression in a K-ras(LSL/+)/Pten(fl/fl) ovarian cancer model. Furthermore, the nanoparticle treatment resulted in reduced systemic and nephrotoxicity, validated by decreased biodistribution of platinum to the kidney as quantified using inductively coupled plasma spectroscopy. Given the universal need for a better platinate, we anticipate this coupling of nanotechnology and structure-activity relationship to rationally reengineer cisplatin could have a major impact globally in the clinical treatment of cancer.</p>10acancer10achemotherapy10ananomedicine1 aParaskar, Abhimanyu, S.1 aSoni, Shivani1 aChin, Kenneth, T.1 aChaudhuri, Padmaparna1 aMuto, Katherine, W.1 aBerkowitz, Julia1 aHandlogten, Michael, W.1 aAlves, Nathan, J.1 aBilgicer, Basar1 aDinulescu, Daniela, M.1 aMashelkar, Raghunath, Anant1 aSengupta, Shiladitya  uhttps://library.ncl.res.in/content/harnessing-structure-activity-relationship-engineer-cisplatin-nanoparticle-enhanced-003013nas a2200409   4500008004100000022001400041245012700055210006900182260008000251300001600331490000800347520160500355653001701960653001701977100002201994700001802016700001802034700002102052700001702073700002002090700002202110700002802132700002002160700002002180700002802200700002202228700002102250700002002271700002902291700002602320700001902346700002702365700002602392700003202418700002502450856012802475       2012                        eng d  a0027-842400aCholesterol-tethered platinum II-based supramolecular nanoparticle increases antitumor efficacy and reduces nephrotoxicity0 aCholesteroltethered platinum IIbased supramolecular nanoparticle  a2101 CONSTITUTION AVE NW, WASHINGTON, DC 20418 USAbNATL ACAD SCIENCEScJUL  a11294-112990 v1093 a<p>Nanoscale drug delivery vehicles have been harnessed extensively as carriers for cancer chemotherapeutics. However, traditional pharmaceutical approaches for nanoformulation have been a challenge with molecules that exhibit incompatible physicochemical properties, such as platinum-based chemotherapeutics. Here we propose a paradigm based on rational design of active molecules that facilitate supramolecular assembly in the nanoscale dimension. Using cisplatin as a template, we describe the synthesis of a unique platinum (II) tethered to a cholesterol backbone via a unique monocarboxylato and O -&gt; Pt coordination environment that facilitates nanoparticle assembly with a fixed ratio of phosphatidylcholine and 1,2-distearoyl-sn-glycero-3-phosphoethanolamine- N-[amino (polyethylene glycol)-2000]. The nanoparticles formed exhibit lower IC50 values compared with carboplatin or cisplatin in vitro, and are active in cisplatin-resistant conditions. Additionally, the nanoparticles exhibit significantly enhanced in vivo antitumor efficacy in murine 4T1 breast cancer and in K-Ras(LSL/+/)Pten(fl/fl) ovarian cancer models with decreased systemic- and nephro-toxicity. Our results indicate that integrating rational drug design and supramolecular nanochemistry can emerge as a powerful strategy for drug development. Furthermore, given that platinum-based chemotherapeutics form the frontline therapy for a broad range of cancers, the increased efficacy and toxicity profile indicate the constructed nanostructure could translate into a nextgeneration platinum-based agent in the clinics.</p>10achemotherapy10ananomedicine1 aSengupta, Poulomi1 aBasu, Sudipta1 aSoni, Shivani1 aPandey, Ambarish1 aRoy, Bhaskar1 aOh, Michael, S.1 aChin, Kenneth, T.1 aParaskar, Abhimanyu, S.1 aSarangi, Sasmit1 aConnor, Yamicia1 aSabbisetti, Venkata, S.1 aKopparam, Jawahar1 aKulkarni, Ashish1 aMuto, Katherine1 aAmarasiriwardena, Chitra1 aJayawardene, Innocent1 aLupoli, Nicola1 aDinulescu, Daniela, M.1 aBonventre, Joseph, V.1 aMashelkar, Raghunath, Anant1 aSengupta, Shiladitya  uhttps://library.ncl.res.in/content/cholesterol-tethered-platinum-ii-based-supramolecular-nanoparticle-increases-antitumor-0