Anticancer Agents

This book is a printed edition of the Special Issue entitled “Anticancer Agents: Design, Synthesis and Evaluation” that was published in Molecules. Two review articles and thirty research papers are included in the Special Issue. Three second-generation androgen receptor antagonists that have been a...

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collection Directory of Open Access Books
description This book is a printed edition of the Special Issue entitled “Anticancer Agents: Design, Synthesis and Evaluation” that was published in Molecules. Two review articles and thirty research papers are included in the Special Issue. Three second-generation androgen receptor antagonists that have been approved by the U.S. FDA for the treatment of prostate cancer have been reviewed. Identification of mimics of protein partners as protein-protein interaction inhibitors via virtual screening has been summarized and discussed. Anticancer agents targeting various protein targets, including IGF-1R, Src, protein kinase, aromatase, HDAC, PARP, Toll-Like receptor, c-Met, PI3Kdelta, topoisomerase II, p53, and indoleamine 2,3-dioxygenase, have been explored. The analogs of three well-known tubulin-interacting natural products, paclitaxel, zampanolide, and colchicine, have been designed, synthesized, and evaluated. Several anticancer agents representing diverse chemical scaffolds were assessed in different kinds of cancer cell models. The capability of some anticancer agents to overcome the resistance to currently available drugs was also studied. In addition to looking into the in vitro ability of the anticancer agents to inhibit cancer cell proliferation, apoptosis, and cell cycle, in vivo antitumor efficacy in animal models and DFT were also investigated in some papers.
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spelling doab-20.500.12854ir-684292024-03-31T13:10:16Z Anticancer Agents Chen, Qiao-Hong benzofurans chemical synthesis cytotoxic properties HeLa MOLT-4 K562 anticancer anti-neuroinflammation coumarin dihydroartemisinin flavonoids allene E-stereoselective regioselective anti-cancer activity cyanopyridone substituted pyridine pyridotriazine pyrazolopyridine thioxotriazopyridine anticancer activity HepG2 antitumor activity computational docking MDM2-p53 interaction xanthones yeast-based assays estrone derivatives hydrazine N-substituted pyrazoline anti-ovarian cancer topoisomerase II inhibitor kinase inhibitor antiproliferative agent urea synthesis antiproliferative activity apoptosis indoleamine 2,3-dioxygenase inhibitor anti-tumor immune modulation tryptophan metabolism taxoids βIII-tubulin P-glycoprotein drug resistance thiopene thienopyrimidinone thiazolidinone breast cancer benzofuran–pyrazole nanoparticles cytotoxic activity PARP-1 inhibition 3,6-dibromocarbazole 5-bromoindole carbazole actin migration Thienopyrimidine Pyrazole PI3Kα inhibitor quinazolin-4(3H)-one quinazolin-4(3H)-thione Schiff base antioxidant activity DFT study ortho-quinones beta-lapachone tanshione IIA PI3Ks PI3Kδ inhibitors 2H-benzo[e][1,2,4]thiadiazine 1,1-dioxide anticancer agents protein–protein interactions virtual screening mimetics drug discovery bivalency polyvalency antitumor cell cycle ovarian cancer P-MAPA IL-12 TLR signaling inflammation chemoresistance 4-(pyridin-4-yloxy)benzamide 1,2,3-triazole c-Met natural product anticancer agent zampanolide Talazoparib PARP inhibitor prodrug o-nitro-benzyl photoactivatable protecting groups salinomycin overcoming drug resistance tumor specificity synergy 5-fluorouracil gemcitabine amides/esters colchicine analogs thiocolchicine colchiceine antimitotic agents hydrates dihydropyranoindole HDAC inhibitors neuroblastoma aromatase MCF-7 NIH3T3 benzimidazole triazolothiadiazine docking ADME organosilicon compounds SILA-409 (Alis-409) SILA-421 (Alis-421) multidrug resistance (MDR) reversal ABCB1 (P-glycoprotein) colon cancer colchicine amide colchicine sulfonamide tubulin inhibitors docking studies crystal structure PROTACs protein degradation IGF-1R Src protein kinase phenylpyrazolopyrimidine enzyme inhibition molecular simulation androgen receptor prostate cancer enzalutamide apalutamide darolutamide triple-negative breast cancer cytotoxicity chrysin analogues flavonoid anticancer compounds thema EDItEUR::M Medicine and Nursing This book is a printed edition of the Special Issue entitled “Anticancer Agents: Design, Synthesis and Evaluation” that was published in Molecules. Two review articles and thirty research papers are included in the Special Issue. Three second-generation androgen receptor antagonists that have been approved by the U.S. FDA for the treatment of prostate cancer have been reviewed. Identification of mimics of protein partners as protein-protein interaction inhibitors via virtual screening has been summarized and discussed. Anticancer agents targeting various protein targets, including IGF-1R, Src, protein kinase, aromatase, HDAC, PARP, Toll-Like receptor, c-Met, PI3Kdelta, topoisomerase II, p53, and indoleamine 2,3-dioxygenase, have been explored. The analogs of three well-known tubulin-interacting natural products, paclitaxel, zampanolide, and colchicine, have been designed, synthesized, and evaluated. Several anticancer agents representing diverse chemical scaffolds were assessed in different kinds of cancer cell models. The capability of some anticancer agents to overcome the resistance to currently available drugs was also studied. In addition to looking into the in vitro ability of the anticancer agents to inhibit cancer cell proliferation, apoptosis, and cell cycle, in vivo antitumor efficacy in animal models and DFT were also investigated in some papers. 2021-05-01T15:09:30Z 2021-05-01T15:09:30Z 2021 book ONIX_20210501_9783036501406_175 9783036501406 9783036501413 https://directory.doabooks.org/handle/20.500.12854/68429 eng application/octet-stream Attribution 4.0 International https://mdpi.com/books/pdfview/book/3445 https://mdpi.com/books/pdfview/book/3445 MDPI - Multidisciplinary Digital Publishing Institute 10.3390/books978-3-0365-0141-3 10.3390/books978-3-0365-0141-3 46cabcaa-dd94-4bfe-87b4-55023c1b36d0 9783036501406 9783036501413 606 Basel, Switzerland open access
spellingShingle benzofurans
chemical synthesis
cytotoxic properties
HeLa
MOLT-4
K562
anticancer
anti-neuroinflammation
coumarin
dihydroartemisinin
flavonoids
allene
E-stereoselective
regioselective
anti-cancer activity
cyanopyridone
substituted pyridine
pyridotriazine
pyrazolopyridine
thioxotriazopyridine
anticancer activity
HepG2
antitumor activity
computational docking
MDM2-p53 interaction
xanthones
yeast-based assays
estrone derivatives
hydrazine
N-substituted pyrazoline
anti-ovarian cancer
topoisomerase II inhibitor
kinase inhibitor
antiproliferative agent
urea
synthesis
antiproliferative activity
apoptosis
indoleamine 2,3-dioxygenase
inhibitor
anti-tumor
immune modulation
tryptophan metabolism
taxoids
βIII-tubulin
P-glycoprotein
drug resistance
thiopene
thienopyrimidinone
thiazolidinone
breast cancer
benzofuran–pyrazole
nanoparticles
cytotoxic activity
PARP-1 inhibition
3,6-dibromocarbazole
5-bromoindole
carbazole
actin
migration
Thienopyrimidine
Pyrazole
PI3Kα inhibitor
quinazolin-4(3H)-one
quinazolin-4(3H)-thione
Schiff base
antioxidant activity
DFT study
ortho-quinones
beta-lapachone
tanshione IIA
PI3Ks
PI3Kδ inhibitors
2H-benzo[e][1,2,4]thiadiazine 1,1-dioxide
anticancer agents
protein–protein interactions
virtual screening
mimetics
drug discovery
bivalency
polyvalency
antitumor
cell cycle
ovarian cancer
P-MAPA
IL-12
TLR signaling
inflammation
chemoresistance
4-(pyridin-4-yloxy)benzamide
1,2,3-triazole
c-Met
natural product
anticancer agent
zampanolide
Talazoparib
PARP inhibitor
prodrug
o-nitro-benzyl
photoactivatable protecting groups
salinomycin
overcoming drug resistance
tumor specificity
synergy
5-fluorouracil
gemcitabine
amides/esters
colchicine analogs
thiocolchicine
colchiceine
antimitotic agents
hydrates
dihydropyranoindole
HDAC inhibitors
neuroblastoma
aromatase
MCF-7
NIH3T3
benzimidazole
triazolothiadiazine
docking
ADME
organosilicon compounds
SILA-409 (Alis-409)
SILA-421 (Alis-421)
multidrug resistance (MDR) reversal
ABCB1 (P-glycoprotein)
colon cancer
colchicine amide
colchicine sulfonamide
tubulin inhibitors
docking studies
crystal structure
PROTACs
protein degradation
IGF-1R
Src
protein kinase
phenylpyrazolopyrimidine
enzyme inhibition
molecular simulation
androgen receptor
prostate cancer
enzalutamide
apalutamide
darolutamide
triple-negative breast cancer
cytotoxicity
chrysin analogues
flavonoid
anticancer compounds
thema EDItEUR::M Medicine and Nursing
Anticancer Agents
title Anticancer Agents
title_full Anticancer Agents
title_fullStr Anticancer Agents
title_full_unstemmed Anticancer Agents
title_short Anticancer Agents
title_sort anticancer agents
topic benzofurans
chemical synthesis
cytotoxic properties
HeLa
MOLT-4
K562
anticancer
anti-neuroinflammation
coumarin
dihydroartemisinin
flavonoids
allene
E-stereoselective
regioselective
anti-cancer activity
cyanopyridone
substituted pyridine
pyridotriazine
pyrazolopyridine
thioxotriazopyridine
anticancer activity
HepG2
antitumor activity
computational docking
MDM2-p53 interaction
xanthones
yeast-based assays
estrone derivatives
hydrazine
N-substituted pyrazoline
anti-ovarian cancer
topoisomerase II inhibitor
kinase inhibitor
antiproliferative agent
urea
synthesis
antiproliferative activity
apoptosis
indoleamine 2,3-dioxygenase
inhibitor
anti-tumor
immune modulation
tryptophan metabolism
taxoids
βIII-tubulin
P-glycoprotein
drug resistance
thiopene
thienopyrimidinone
thiazolidinone
breast cancer
benzofuran–pyrazole
nanoparticles
cytotoxic activity
PARP-1 inhibition
3,6-dibromocarbazole
5-bromoindole
carbazole
actin
migration
Thienopyrimidine
Pyrazole
PI3Kα inhibitor
quinazolin-4(3H)-one
quinazolin-4(3H)-thione
Schiff base
antioxidant activity
DFT study
ortho-quinones
beta-lapachone
tanshione IIA
PI3Ks
PI3Kδ inhibitors
2H-benzo[e][1,2,4]thiadiazine 1,1-dioxide
anticancer agents
protein–protein interactions
virtual screening
mimetics
drug discovery
bivalency
polyvalency
antitumor
cell cycle
ovarian cancer
P-MAPA
IL-12
TLR signaling
inflammation
chemoresistance
4-(pyridin-4-yloxy)benzamide
1,2,3-triazole
c-Met
natural product
anticancer agent
zampanolide
Talazoparib
PARP inhibitor
prodrug
o-nitro-benzyl
photoactivatable protecting groups
salinomycin
overcoming drug resistance
tumor specificity
synergy
5-fluorouracil
gemcitabine
amides/esters
colchicine analogs
thiocolchicine
colchiceine
antimitotic agents
hydrates
dihydropyranoindole
HDAC inhibitors
neuroblastoma
aromatase
MCF-7
NIH3T3
benzimidazole
triazolothiadiazine
docking
ADME
organosilicon compounds
SILA-409 (Alis-409)
SILA-421 (Alis-421)
multidrug resistance (MDR) reversal
ABCB1 (P-glycoprotein)
colon cancer
colchicine amide
colchicine sulfonamide
tubulin inhibitors
docking studies
crystal structure
PROTACs
protein degradation
IGF-1R
Src
protein kinase
phenylpyrazolopyrimidine
enzyme inhibition
molecular simulation
androgen receptor
prostate cancer
enzalutamide
apalutamide
darolutamide
triple-negative breast cancer
cytotoxicity
chrysin analogues
flavonoid
anticancer compounds
thema EDItEUR::M Medicine and Nursing
topic_facet benzofurans
chemical synthesis
cytotoxic properties
HeLa
MOLT-4
K562
anticancer
anti-neuroinflammation
coumarin
dihydroartemisinin
flavonoids
allene
E-stereoselective
regioselective
anti-cancer activity
cyanopyridone
substituted pyridine
pyridotriazine
pyrazolopyridine
thioxotriazopyridine
anticancer activity
HepG2
antitumor activity
computational docking
MDM2-p53 interaction
xanthones
yeast-based assays
estrone derivatives
hydrazine
N-substituted pyrazoline
anti-ovarian cancer
topoisomerase II inhibitor
kinase inhibitor
antiproliferative agent
urea
synthesis
antiproliferative activity
apoptosis
indoleamine 2,3-dioxygenase
inhibitor
anti-tumor
immune modulation
tryptophan metabolism
taxoids
βIII-tubulin
P-glycoprotein
drug resistance
thiopene
thienopyrimidinone
thiazolidinone
breast cancer
benzofuran–pyrazole
nanoparticles
cytotoxic activity
PARP-1 inhibition
3,6-dibromocarbazole
5-bromoindole
carbazole
actin
migration
Thienopyrimidine
Pyrazole
PI3Kα inhibitor
quinazolin-4(3H)-one
quinazolin-4(3H)-thione
Schiff base
antioxidant activity
DFT study
ortho-quinones
beta-lapachone
tanshione IIA
PI3Ks
PI3Kδ inhibitors
2H-benzo[e][1,2,4]thiadiazine 1,1-dioxide
anticancer agents
protein–protein interactions
virtual screening
mimetics
drug discovery
bivalency
polyvalency
antitumor
cell cycle
ovarian cancer
P-MAPA
IL-12
TLR signaling
inflammation
chemoresistance
4-(pyridin-4-yloxy)benzamide
1,2,3-triazole
c-Met
natural product
anticancer agent
zampanolide
Talazoparib
PARP inhibitor
prodrug
o-nitro-benzyl
photoactivatable protecting groups
salinomycin
overcoming drug resistance
tumor specificity
synergy
5-fluorouracil
gemcitabine
amides/esters
colchicine analogs
thiocolchicine
colchiceine
antimitotic agents
hydrates
dihydropyranoindole
HDAC inhibitors
neuroblastoma
aromatase
MCF-7
NIH3T3
benzimidazole
triazolothiadiazine
docking
ADME
organosilicon compounds
SILA-409 (Alis-409)
SILA-421 (Alis-421)
multidrug resistance (MDR) reversal
ABCB1 (P-glycoprotein)
colon cancer
colchicine amide
colchicine sulfonamide
tubulin inhibitors
docking studies
crystal structure
PROTACs
protein degradation
IGF-1R
Src
protein kinase
phenylpyrazolopyrimidine
enzyme inhibition
molecular simulation
androgen receptor
prostate cancer
enzalutamide
apalutamide
darolutamide
triple-negative breast cancer
cytotoxicity
chrysin analogues
flavonoid
anticancer compounds
thema EDItEUR::M Medicine and Nursing
url ONIX_20210501_9783036501406_175