LEADER 04558nam 22006735 450 001 9910254023703321 005 20200704082049.0 010 $a981-10-0657-1 024 7 $a10.1007/978-981-10-0657-9 035 $a(CKB)3710000000602246 035 $a(EBL)4415589 035 $a(SSID)ssj0001653295 035 $a(PQKBManifestationID)16433721 035 $a(PQKBTitleCode)TC0001653295 035 $a(PQKBWorkID)14983096 035 $a(PQKB)10780484 035 $a(DE-He213)978-981-10-0657-9 035 $a(MiAaPQ)EBC4415589 035 $a(PPN)192222996 035 $a(EXLCZ)993710000000602246 100 $a20160219d2016 u| 0 101 0 $aeng 135 $aur|n|---||||| 181 $ctxt 182 $cc 183 $acr 200 10$aAnti-Cancer N-Heterocyclic Carbene Complexes of Gold(III), Gold(I) and Platinum(II) $eThiol ?Switch-on? Fluorescent Probes, Thioredoxin Reductase Inhibitors and Endoplasmic Reticulum Targeting Agents /$fby Taotao Zou 205 $a1st ed. 2016. 210 1$aSingapore :$cSpringer Singapore :$cImprint: Springer,$d2016. 215 $a1 online resource (175 p.) 225 1 $aSpringer Theses, Recognizing Outstanding Ph.D. Research,$x2190-5053 300 $aDescription based upon print version of record. 311 $a981-10-0656-3 320 $aIncludes bibliographical references. 327 $aIntroduction -- Experimental Section -- Gold(III) Complexes Containing N-Heterocyclic Carbene Ligand Serve as Dual Fluorescent Thiol ?Switch-on? Probe and Anti-Cancer Agent -- A Binuclear Gold(I) Complex with Mixed Bridging Diphosphine and Bis(N-Heterocyclic Carbene) Ligands Shows Favorable Thiol Reactivity and Effectively Inhibits Tumor Growth and Angiogenesis in Vivo -- Luminescent Organoplatinum(II) Complexes Containing Bis(N-Heterocyclic Carbene) Ligands Selectively Target Endoplasmic Reticulum and Induce Potent Phototoxicity -- Summary and Evaluation. 330 $aThis thesis focuses on the development of gold- and non-classical platinum-based anti-cancer agents that display distinctively different anti-cancer mechanisms compared to the commonly used cisplatin. These metal complexes contain N-heterocyclic carbene (NHC) ligands which are able to form strong M-C(NHC) bonds, conferring high stability and favorable lipophilicity, reactivity and binding specificity of metal complexes on biomolecules. The author demonstrates significant advances made in anti-cancer gold(III), gold(I) and platinum(II) complexes. Detailed chemical synthesis, in vitro and/or in vivo anti-cancer activities are clearly presented including: (i) a class of Au(III) complexes containing a highly fluorescent N^N^N ligand and NHC ligand that simultaneously act as fluorescent thiol ?switch-on? probes and anti-cancer agents; (ii) a dinuclear gold(I) complex with a mixed diphosphine and bis(NHC) ligand displaying favorable stability and showing significant inhibition of tumor growth in two independent mice models with no observable side effects; and (iii) a panel of stable luminescent cyclometalated platinum(II) complexes exhibiting high specificity to localize to the endoplasmic reticulum (ER) domain, inducing ER stress and cell apoptosis. These works highlight the clinical potential that gold and platinum complexes offer for cancer treatment. 410 0$aSpringer Theses, Recognizing Outstanding Ph.D. Research,$x2190-5053 606 $aInorganic chemistry 606 $aMedicinal chemistry 606 $aMolecular biology 606 $aCancer research 606 $aInorganic Chemistry$3https://scigraph.springernature.com/ontologies/product-market-codes/C16008 606 $aMedicinal Chemistry$3https://scigraph.springernature.com/ontologies/product-market-codes/C28000 606 $aMolecular Medicine$3https://scigraph.springernature.com/ontologies/product-market-codes/B1700X 606 $aCancer Research$3https://scigraph.springernature.com/ontologies/product-market-codes/B11001 615 0$aInorganic chemistry. 615 0$aMedicinal chemistry. 615 0$aMolecular biology. 615 0$aCancer research. 615 14$aInorganic Chemistry. 615 24$aMedicinal Chemistry. 615 24$aMolecular Medicine. 615 24$aCancer Research. 676 $a540 700 $aZou$b Taotao$4aut$4http://id.loc.gov/vocabulary/relators/aut$01062282 906 $aBOOK 912 $a9910254023703321 996 $aAnti-Cancer N-Heterocyclic Carbene Complexes of Gold(III), Gold(I) and Platinum(II)$92524149 997 $aUNINA