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Index

Note: Page numbers in italic refers to gures/schemes.

abecarnil 58 activities of β- carbolines 52– 53

see also antibacterial properties of β- carbolines;

antifungal actions of β- carboline products; antimalarial activity of β- carbolines; antioxidant activity of β- carbolines

anti- HIV agents, biological activities exhibited

by β- carbolines 235– 236 anti- inammatory agents 226– 227 anticancer activity of β- carbolines 3, 31– 44 biological activities exhibited by β- carbolines

235– 236 pharmaceutical activities of β- carbolines 207

Akt kinase 110– 112 alangiobussine synthesis 65 alangiobussinine synthesis 65 Alzheimer’s disease 103, 104 anti- HIV agents 234– 255

biological activities exhibited by β- carbolines

235– 236 discovery and signicance of β- carbolines

236– 237 drug discovery overview 234– 236 drymaritin 240, 243 azin 238, 241, 243– 246 functionalization of the β- carboline scaffold

252– 254 future outlook 254– 255 harman 240, 241 harmine 236 HIV- 1 reverse transcriptase (RT) 243– 244, 247– 249 manzamine alkaloids 61, 241, 242 medicinally important β- carbolines based

compounds 236– 237 natural sources of β- carbolines 237– 238 neurotransmitter interaction 236– 237 scaffolds, importance of 234– 236 structural diversity of carbolines 235 synthesis of β- carbolines 237– 238, 245– 251

anti- inammatory agents, β- carboline as 226– 227 antibacterial properties of β- carbolines 53– 61

synthetic aspects of β- carbolines having

antibacterial property 67– 73

anticancer activity of β- carbolines 3

synthesis of β- carboline derivatives as

anticancer agents 34– 44 targeting multiple biological objectives 31– 34

antidepressant agents, β- carboline as 221– 225 antifungal actions of β- carboline products 88– 90 antifungal mediators, β- carboline products as 85– 88 antimalarial activity of β- carbolines 158– 175

malaria background 158– 160 synthesis of β- carbolines 160– 169 β- carboline derivatives 169– 174

antioxidant activity of β- carbolines 183– 194

dihydro β- carbolines 189 ethyl β- carboline- 3- carboxylate (β- CCE)

190– 193 future aspects 194 pharmacological active β- carbolines 180– 183 reactive oxygen species (ros) 191 recent advances 190– 193 synthetic β- carbolines 190 tetrahydro- β- carbolines 183– 186 β- carboline alkaloids 186– 188

applications of β- carbolines 73– 74 Aurora kinases 117– 118

B- Raf kinase 118

β- carboline alkaloids, antioxidant activity of

β- carbolines 186– 188

β- carboline- combretastatin carboxamide

conjugates 31– 34

β- CCE (ethyl β- carboline- 3- carboxylate),

antioxidant activity of β- carbolines 190– 193

biological activities exhibited by β- carbolines

235– 236

C- 7 position of β- carbolines 146 canthine synthesis 66– 67 CDC- like Kinase 1 (CLK1) 108– 110 CDKs (cyclin- dependent kinases) 23– 24, 96– 101 cell cycle as target, synthesis of β- carboline

derivatives as anticancer agents 29– 31

characteristics of β- carbolines 61– 62 chemical composition of several carboline kinds

204– 206

CLK1 (CDC- like Kinase 1) 108– 110 combilexins, DNA targeting agents 15– 19 compounds with unexplored mechanism of

action, synthesis of β- carboline derivatives as

anticancer agents 34– 44

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cyclic aldimines, synthesis 67 cyclin- dependent kinases (CDKs) 23– 24, 96– 101 cyclometalated Ir (III) complexes 100 cyclometalated Ru(II) complexes 99

HDAC inhibitors, synthesis of β- carboline

derivatives as anticancer agents 26– 29

HIV see anti- HIV agents hybrid β- carbolines 130– 132 hyrtioerectines 61

Index

depression, β- carboline as antidepressant agents

221– 225 derivatives of carboline alkaloids 61, 62 diabetes, kinases inhibitors 103– 104 dihydro β- carbolines 189 discovery and signicance of β- carbolines

236– 237 DNA targeting agents

combilexins 15– 19 DNA groove- binding agents 9– 14 intercalating agents 3– 8 scission 19– 21 synthesis of β- carboline derivatives 3– 21 topoisomerase inhibitors 14– 15 drug discovery overview 234– 236 drymaritin 240, 243

dual- specicity Tyrosine Phosphorylation-

regulated Kinases (DYRKs) 101– 104

epigallocatechin gallate (EGCG) 104 ethyl β- carboline- 3- carboxylate (β- CCE),

antioxidant activity of β- carbolines 190– 193 eudistomins- Y and its analogues 53, 54

fascaplysin 98– 99 azin 238, 241, 243– 246 functionalization of β- carbolines 134– 147,

252– 254 future aspects, antioxidant activity of

β- carbolines 194 future outlook, anti- HIV agents 254– 255 future perspectives, synthesis of β- carboline

derivatives as anticancer agents 44

Glycogen Synthase Kinase (GSK) 115– 116

harmaline 57, 82– 83, 101 harman 240, 241 harmane 55– 56, 60 harmine 82– 83, 96, 102– 103, 236 haspase kinase inhibitors 21– 23 haspin kinase inhibitors 21– 23, 116– 117

IKK (IκB kinase) 107– 108 intercalating agents, DNA targeting agents 3– 8 IκB kinase (IKK) 107– 108

kinases as target

cyclin- dependent kinases (CDKs) 23– 24 haspin kinase inhibitors 21– 23 synthesis of β- carboline derivatives as

anticancer agents 21– 24

kinases inhibitors 94– 120

Akt kinase 110– 112 Alzheimer’s disease 103, 104 Aurora kinases 117– 118 B- Raf kinase 118 CDC- like Kinase 1 (CLK1) 108– 110 cyclin- dependent kinases (CDKs) 23– 24, 96– 101 cyclometalated Ir (III) complexes 100 cyclometalated Ru(II) complexes 99 diabetes 103– 104 dual- specicity Tyrosine Phosphorylation-

regulated Kinases (DYRKs) 101– 104 epigallocatechin gallate (EGCG) 104 fascaplysin 98– 99 Glycogen Synthase Kinase (GSK) 115– 116 harmaline 101 harmine 96, 102– 103 haspin kinase 116– 117 IκB kinase (IKK) 107– 108 manzamine A 100 mezamine A 100 Mitogen- activated Protein Kinase- activated

Protein Kinase 2 (MAPKAPK2) 105– 107 platelet- derived growth factor (PDGF) 118– 119 Polo- like Kinases (PLKs) 113– 115 Protein Kinase B (PKB or Akt) 110– 112 protein tyrosine kinase 6 (PTK6) 118 pyrrolo[2,3- a] carbazole analogs 98 Ru (II)- containing arene entities 99– 100 SK1/ sphingosine- 1- phosphate pathway 119 Suzuki- Miyaura reaction 99 tau phosphorylation 103 tryptamine and tetrahydro- β- C biphenyl

derivatives 99

kinesin (Eg5) inhibitors, synthesis of β- carboline

derivatives as anticancer agents 26

komavine synthesis 65– 66

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Index

malaria see antimalarial activity of β- carbolines manzamine A 100 manzamine alkaloids 61, 241, 242 MAPKAPK2 (Mitogen- activated Protein Kinase-

activated Protein Kinase 2) 105– 107

marine alkaloid oriented β- carboline

synthesis 84– 85

medicinally important β- carbolines based

compounds 236– 237 mezamine A 100 Mitogen- activated Protein Kinase- activated

Protein Kinase 2 (MAPKAPK2) 105– 107

N(2)- substituted β- carbolines 132– 134 natural products having a simple β- carboline

skeleton 63- 67 natural sources of β- carbolines 237– 238 naturally occurring β- carboline alkaloids 95 neamine- carboline conjugates 55 neurotransmitter interaction 236– 237 norharman synthesis 63

occurrence of β- carbolines 62- 63

PDGF (platelet- derived growth factor) 118– 119 pharmaceutical activities of β- carbolines 207 pharmacological active β- carbolines 180– 183 pharmacologically interesting β- carbolines 55, 56 PKB or Akt (Protein Kinase B) 110– 112 plakortamine 60 platelet- derived growth factor (PDGF) 118– 119 Polo- like Kinases (PLKs) 113– 115 Protein Kinase B (PKB or Akt) 110– 112 protein tyrosine kinase 6 (PTK6) 118 pyrrolo[2,3- a] carbazole analogs 98

reactive oxygen species (ROS), antioxidant

activity of β- carbolines 191 Ru (II)- containing arene entities 99– 100

SK1/ sphingosine- 1- phosphate pathway 119 sources of β- carbolines 53– 54 stolonine synthesis 64 structural diversity of carbolines 1– 2, 55– 61, 95,

160, 161, 180, 206– 208, 235 sulfanyl derivatives of β- carbolines 135– 139 sulfone derivatives of β- carbolines 142– 145 sulfur- containing β- carbolines 126– 151

C- 3 functionalization of β- carbolines 134– 145 C- 6 sulfur- containing β- carbolines 145 C- 7 position of β- carbolines 146 drug design 129– 147 hybrid β- carbolines 130– 132 N(2)- substituted β- carbolines 132– 134 S- functionalization at the N(9)- position of

β- carbolines 146– 147

sulfanyl derivatives of β- carbolines 135– 139 sulfone derivatives of β- carbolines 142– 145 synthesis 129– 147 thiocarbamide and thione derivatives of

β- carbolines 139– 142

transition metal complexes involving

β- carbolines as N- ligands 147– 151 Suzuki- Miyaura reaction 99 synthesis of tetrahydro- β- carbolines 163,

218– 221 synthesis of β- carboline derivatives 206– 221 synthesis of β- carboline derivatives as anticancer

agents 3– 44

cell cycle as target 29– 31 compounds with unexplored mechanism of

action 34– 44

DNA targeting agents 3– 21 future perspectives 44 HDAC inhibitors 26– 29 kinases as target 21– 24 kinesin (Eg5) inhibitors 26 targeting multiple biological objectives

31– 34

tubulin/ microtubule as a target 24– 25

synthesis of β- carbolines 64, 65, 238

anti- HIV agents 237– 238, 245– 251 antimalarial activity of β- carbolines 160– 169 marine alkaloid focus 84– 85

synthetic β- carbolines

antioxidant activity 190 having antibacterial property 67– 73

263

S- functionalization at the N(9)- position of

β- carbolines 146– 147 SARs analysis of β- carbolines 180 scaffolds, importance of 234– 236 scission, DNA targeting agents 19– 21 shishijimicin A synthesis 66

tau phosphorylation 103 tetrahydro- β- carbolines 83– 84

antioxidant activity of β- carbolines 183– 186 stereoisomers 170 synthesis 163, 218– 221

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tryptamine and tetrahydro- β- C biphenyl

derivatives 99 tetrahydroharmane synthesis 64– 65 thiocarbamide and thione derivatives of

β- carbolines 139– 142 topoisomerase inhibitors, DNA targeting

agents 14– 15 transition metal complexes involving β- carbolines

as N- ligands 147– 151

tryptamine and tetrahydro- β- C biphenyl

derivatives 99

tubulin/ microtubule as a target, synthesis of

β- carboline derivatives as anticancer agents 24– 25

yohimbine 58– 59

Index

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