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Natural products have been a source of inspiration for chemists and chemical biologists for many years, and have a special relevance in the chemical space. In recent years, several novel synthetic strategies have appeared, such as diversity-oriented synthesis (DOS), biological-oriented synthesis (BiOS), and function-oriented synthesis (FOS), for accessing complex and functionally diverse molecules. In this manner, the synthesis of natural products has evolved towards simpler and ecological methods using biotransformation, combinatorial chemistry, or organocatalysts. In this issue, Prof. Chojnacka shows demonstrates the use of immobilized lipases as catalysts to aid in the synthesis of phosphatidylcholine enriched with myristic acid. Profs. Vila and Pedro used catalysts derived from (S)-mandelic acid to achieve the catalytic enantioselective addition of dimethylzinc to isatins. Prof. Diez shows the possibility of the obtention of 7,8-carvone epoxides in a diastereoselective manner using proline, quinidine, and diphenylprolinol as organocatalysts. A cheap, simple, clean, and scalable method involves the use of deep eutectic mixtures as reaction media, and Profs. Alonso and Guillena describe the use of this methodology for the enantioselective, organocatalyzed ?-amination of 1,3-dicarbonyl compounds. Biotransformations have been one of the methodologies for more efficient synthesis of natural products. Prof. Wu transforms ergostane triterpenoid antcin K using Psychrobacillus sp. Ak 187. Finally, Prof. Kovayashi reviews the total synthesis and biological evaluation of phaeosphaerides. The reader, through this issue, could gain an idea of the new directions that the synthesis of natural products using catalysts will have in the years to come.

n/a --- structured phosphatidylcholine --- carvone --- immobilized lipases --- trimyristin --- 3-hydroxyoxindole --- green chemistry --- structural revision --- anticancer --- triterpenoid --- organocatalysis --- natural products --- epoxidation --- ?-amination --- benzimidazole --- total synthesis --- zinc --- Antrodia cinnamomea --- aminocatalysis --- epoxide --- asymmetric organocatalysis --- mandelamides --- STAT3 --- asymmetric catalysis --- Psychrobacillus --- isatin --- chiral ?-hydroxyamide --- interesterification --- proline --- phaeosphaeride B --- biotransformation --- phaeosphaeride A --- myristic acid --- egg-yolk phosphatidylcholine --- acidolysis --- antcin K --- deep eutectic solvents

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Patient outcomes remain poor for many cancers despite improvements in treatments and new molecular-targeted biomedicines for certain cancer types or subtypes. Dose-limiting toxicity, a narrow therapeutic index, and the development of resistance to traditional anti-cancer agents are well-established. It is apparent that inherent and acquired drug resistance are major challenges with molecular-targeted agents and that on- as well as off-target side effects can still occur. Other issues include drug metabolism by the body and safely supplying a sufficient amount of active drug to the tumor cells. There is a clear and urgent need for new molecular targets and drugs that specifically target cancer cells in different ways to existing approved drugs. This book, through a collection of eight research articles and two review articles from the Biomedicines themed Special Issue ‘Novel Anti-Cancer Agents and Cellular Targets and Their Mechanism(s) of Action’, provides a snapshot of some of the diverse and exciting research approaches being taken by the cancer research community in trying to address some of these therapeutic challenges.

Technology: general issues --- History of engineering & technology --- microtubule acetylation --- triple-negative breast cancer --- anti-cancer agent --- apoptosis --- K562 --- 8-hydroxydaidzein --- autophagy --- BCR-ABL --- MAPK --- NF-κB --- c-myc --- RNA interference --- siRNA --- oncogene --- gene silencing --- expression --- nanosystems --- Cytochrome P450 --- CYP1A1 --- CYP1B1 --- CYP2W1 --- breast cancer --- prodrug --- bioprecursor --- duocarmycin --- phortress --- AQ4N --- 5-FU resistance --- colorectal cancer --- drug repurposing --- Genomics of Drug Sensitivity in Cancer --- Connectivity Map --- anticancer drug --- B-lactam steroid alkylators --- synthetic lethality --- poly (ADP-ribose) polymerase inhibitors --- ovarian cancer --- hybrid steroidal alkylating agents --- migration --- invasion --- glioblastoma --- CCN1 --- mesenchymal–amoeboid transition --- biomarker --- HepG2 --- Huh7 --- isatin sulfonamides --- angiogenesis --- cancer hallmarks --- molecular docking --- EGFR tyrosine kinase inhibitor --- photon upconversion --- triplet-triplet annihilation --- in vivo imaging --- PLGA --- nanoparticles --- affibody molecule --- human epidermal growth factor receptor 3 (HER3) --- BxPC-3 --- emtansine --- DM1 --- albumin binding domain --- affibody drug conjugate (AffiDC) --- n/a --- mesenchymal-amoeboid transition

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The word "cancer" is associated with at least 100 different pathologies, depending on the organ involved and the type of tumor developed. Cancer is a complex disease involving multiple pathogenetic mechanisms. Characterization of different types of cancers, which distinguishes them from healthy cells and other cancers, allows for the identification of specific targets for each individual tumor. The principle of chemotherapy is based on interference with the mechanisms that regulate the life and proliferation of cancer cells, causing their death. In recent years, there has been continuous progress in the development of therapeutic agents against cancer, which is ongoing.The Anticancer Inhibitors Special Issue focuses on new target-based anticancer agents that inhibit a specific target involved in the suppression of various types of cancer and the control of their chemoresistance.There is a collection of research and review articles on advances in drug discovery, design, and development of new inhibitor compounds with potency against various cancer types.

Research & information: general --- Chemistry --- breast cancer --- tamoxifen --- LY294002 --- synergism --- apoptosis --- cell cycle --- tea (Camellia sinensis) flowers --- BTFS --- A2780/CP70 ovarian cancer cells --- S phase cell cycle arrest --- nicotinamide phosphoribosyltransferase --- NAD+ biosynthesis --- inhibitor --- azacyclohexane --- anticancer drug --- drug design --- enthalpy effect --- NSCLC --- Cathepsin K --- cell proliferation --- cell migration --- cell invasion --- mTOR --- isatin-hydrazones --- cytotoxicity --- CDK2 inhibitor --- ATP competitive inhibitor --- ADME analysis --- receptor tyrosine kinases --- protein-protein interactions --- protein engineering --- directed evolution --- angiogenesis --- binding affinity --- agonistic activity --- saponins --- phytochemicals --- tea (Camellia sinensis) flower --- ovarian cancer --- autophagy --- ZMYND8 --- tumorigenesis --- epigenetic regulation --- pro-oncogenic effects --- tumor suppression --- tacrine-coumarin derivatives --- DNA --- topoisomerases I, II --- lung carcinoma cells --- A549 --- chemotherapy --- prodrug --- drug targeting --- overexpressed enzymes --- ADC --- ADEPT --- GDEPT --- LEAPT --- PROTAC --- cyclin-dependent kinase --- cancer --- resistance --- small molecule inhibitors --- PROTACs --- statins --- pancreatic cancer --- DNA microarray --- pitavastatin --- cerivastatin --- simvastatin --- fluvastatin --- atorvastatin --- pravastatin --- HMG-CoA reductase inhibitors --- n/a

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The very first marine-derived anticancer drug, Cytarabine (aka Ara-C, Cytosar-U®), was approved by the FDA in 1969 for the treatment of leukemia. At the beginning of 2021, the list of approved marine-derived anticancer drugs consists of nine substances, five of which received approval within the last two years, demonstrating the rapid evolution of the field. The current book is a collection of scientific articles related to the exponentially growing field of anticancer marine compounds. These articles cover the whole field, from agents with cancer-preventive activity, to novel and previously characterized compounds with anticancer activity, both in vitro and in vivo, as well as the latest status of compounds under clinical development.

Medicine --- apoptosis --- fucoidan --- hepatocellular carcinoma --- reactive oxygen species --- 3-alkylpyridinium polymers --- nicotine --- nicotinic acetylcholine receptor --- non-small cell lung carcinoma --- melanoma --- sinulariolide --- proteomic --- mitochondria --- caspase cascade --- marine fungus --- sediment --- anthranilic acid --- Penicillium paneum --- cytotoxicity --- dibromotyrosine --- mitochondrial dysfunction --- oxidative stress --- topoisomerase --- epigonal organ --- bonnethead shark --- Jurkat --- tumor cell line --- hippuristanol --- PEL --- AP-1 --- STAT3 --- Akt --- colorectal cancer --- marine mollusc --- brominated indoles --- shrimp --- chemoprevention --- fatty acids --- carotenoids --- cancer --- nanoparticle --- osteosarcoma --- lung metastasis --- elisidepsin --- lipid rafts --- hydroxylated lipids --- fatty acid 2-hydroxylase --- cooperative binding --- membrane permeabilization --- marine organisms --- polysaccharides --- anticancer --- anticarcinogenic --- mechanisms of action --- fumigaclavine C --- anti-proliferation --- mitochondrial pathway --- anti-cancer --- anti-proliferative --- carotenoid --- cell cycle arrest --- fucoxanthin --- azoxymethane --- bioactive natural product --- isatin --- in vivo model --- Marthasterias glacialis L. --- palmitic acid --- ER-stress --- CHOP --- Antibody Drug Conjugates (ADCs) --- marine antitumor agents --- clinical trials --- approved antitumor agents --- AD0157 --- angiogenesis --- marine drug --- pyrrolidinedione --- secondary metabolites --- cancer preventive --- chemopreventive --- trabectedin --- plitidepsin --- tumor-associated macrophages --- tumor microenvironment --- preclinical --- anticancer immunity --- antiangiogenesis --- fascaplysin --- cyclin-dependent kinase --- small cell lung cancer --- camptothecin --- poly(ADP-ribose)-polymerase inhibitor --- breast cancer --- seaweed --- therapeutic compounds --- autophagy --- marine drugs --- autophagy inhibitors --- autophagy inducers --- macrolide --- programmed cell death --- energy stress --- araguspongine C --- c-Met --- HER2 --- gemcitabine --- pazopanib --- phase I --- safety --- soft tissue sarcoma --- pachastrissamine --- jaspine B --- carbocyclic analogue --- sphingosine kinase inhibitor --- molecular modeling --- ET-743 --- DNA minor groove binder --- chemotherapy --- bis (2,3-dibromo-4,5-dihydroxy-phenyl)-methane (BDDPM) --- anti-metastatic activity --- cell adhesion --- β1-integrin --- FAK --- BEL-7402 cell --- triterpene glycosides --- sea cucumbers --- antitumor activities --- arrest of cell cycle --- antibacterial --- marangucyclines --- deep-sea --- Streptomyces sp. SCSIO 11594 --- LS-1 --- SNU-C5/5-FU --- TGF-β signaling --- carcinoembryonic antigen --- kalkitoxin --- Moorea producens --- mitochondria toxin --- VEGF --- angiogenesis inhibitor --- hypoxia-inducible factor-1 --- HIF-1 --- Lyngbya majuscula --- marine metabolites --- SZ-685C --- nonfunctioning pituitary adenomas --- Ecklonia cava --- phlorotannins --- dieckol --- migration --- sipholenol A --- ABC transporter --- multidrug resistance --- P-gp/ABCB1 --- BCRP/ABCG2 --- MRP1/ABCC1 --- marine natural products --- glioblastoma --- xyloketal B --- proliferation --- TRPM7 --- marine compound --- ribosomal protein genes --- snoRNA --- FAU --- RPS30 --- SNORA62 --- evolution --- Porifera --- n/a --- Penicillium brevicompactum --- Brevianamide --- Mycochromenic acid derivative --- antifouling --- Caribbean sponge --- plakortide --- endoperoxide --- leukemia --- multi-drug resistant leukemia --- Sarcophyton ehrenbergi --- soft coral --- terpenes --- cembranoids --- cytotoxic activity --- molecular docking --- uveal melanoma --- virtual screening --- Topo I inhibitor --- low toxic --- natural product --- Ulva fasciata --- selenium-containing polysaccharide-protein complex --- pseudopterosin --- NF-κB --- p65 --- inflammation --- cytokine release --- IL-6 --- TNFα --- MCP-1 --- glucocorticoid receptor --- paulomycins --- Micromonospora --- antitumor --- Cantabrian Sea-derived actinobacteria --- puupehenones --- sponges --- antiangiogenic --- antitumoral --- porifera/sponge --- cancer genes --- molecular oncology --- bromophenol --- molecular mechanisms --- cell cycle --- PI3K/Akt --- p38/ERK --- ROS --- human lung cancer --- glycosaminoglycans --- antiproliferative --- heparan sulphate --- gliotoxin --- NSCLC --- adriamycin resistance --- Sepia ink polysaccharides --- antitumour --- chemosensitization --- anticoagulation --- sea anemone --- drug discovery --- endothelial cells --- RGD motif --- kunitz type inhibitor --- prostate cancer --- antioxidant --- natural marine compounds --- marine biotechnology --- microalgae --- marine sponges --- Aeroplysinin --- Isofistularin --- pheochromocytoma and paraganglioma --- metastasis --- cancer progression --- cell adhesion molecules --- integrin β1 --- hypoxia --- phycocyanin --- non-small cell lung cancer --- NF-κB signaling --- marine-derived drugs --- bioanalysis --- chromatography --- manzamine A --- epithelial–mesenchymal transition --- lung cancer --- circulating tumor cells --- signal transduction --- cisplatin --- Lampetra morii --- buccal gland --- cystatin F --- anti-angiogenesis --- cystatin superfamily --- Antimicrobial peptide (AMP) --- Tilapia piscidin 4 (TP4) --- non-small cell lung cancer (NSCLC) --- itampolin A --- FBDD --- p38α --- novel inhibitor --- tetracenomycin X --- cyclin D1 --- proteasomal degradation --- p38 --- c-JUN --- λ-carrageenan --- heparanase --- anticoagulant --- depolymerisation --- cell migration --- Aspergillus --- naphthopyrones --- endophytic fungus --- Leathesia nana --- mangrove-derived actinomycete --- ansamycins --- divergolides --- apoptosis-inducing activity --- actinomycin --- EMT --- invasion --- low molecular weight fucoidan extract --- N-Ras --- neuroblastoma-rat sarcoma --- Cancer --- programmed cell death-ligand 1 --- programmed cell death-ligand 2 --- human sarcoma cell line (HT1080 cells) --- human normal diploid fibroblast (TIG-1 cells) --- chimera --- chemical conjugation --- anticancer agent --- hybridization --- α9-nicotinic acetylcholine receptors (nAChRs) --- breast cancer cells --- αO-conotoxin GeXIVA --- targeted therapy --- gorgonian --- Leptogorgia --- humulane sesquiterpenoids --- anticancer activity --- 12-deacetyl-12-epi-scalaradial --- HeLa cells --- Nur77 --- MAPK/ERK pathway --- Mycalin A --- C15 acetogenins --- synthetic analogues --- antiproliferative activity --- A375 and HeLa cell lines --- polyoxygenated steroids --- sponge --- Haliclona gracilis --- Thalassia testudinum --- thalassiolin B --- polyphenols --- CYP1A1 --- benzo[a]pyrene --- JNK1/2 --- natural products --- synergism --- A549 cells --- cytoskeleton --- P2X7 receptor --- pollution --- anti-angiogenic --- gene expression --- HSP90 --- inhibitor --- epithelial-mesenchymal transition

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The very first marine-derived anticancer drug, Cytarabine (aka Ara-C, Cytosar-U®), was approved by the FDA in 1969 for the treatment of leukemia. At the beginning of 2021, the list of approved marine-derived anticancer drugs consists of nine substances, five of which received approval within the last two years, demonstrating the rapid evolution of the field. The current book is a collection of scientific articles related to the exponentially growing field of anticancer marine compounds. These articles cover the whole field, from agents with cancer-preventive activity, to novel and previously characterized compounds with anticancer activity, both in vitro and in vivo, as well as the latest status of compounds under clinical development.

apoptosis --- fucoidan --- hepatocellular carcinoma --- reactive oxygen species --- 3-alkylpyridinium polymers --- nicotine --- nicotinic acetylcholine receptor --- non-small cell lung carcinoma --- melanoma --- sinulariolide --- proteomic --- mitochondria --- caspase cascade --- marine fungus --- sediment --- anthranilic acid --- Penicillium paneum --- cytotoxicity --- dibromotyrosine --- mitochondrial dysfunction --- oxidative stress --- topoisomerase --- epigonal organ --- bonnethead shark --- Jurkat --- tumor cell line --- hippuristanol --- PEL --- AP-1 --- STAT3 --- Akt --- colorectal cancer --- marine mollusc --- brominated indoles --- shrimp --- chemoprevention --- fatty acids --- carotenoids --- cancer --- nanoparticle --- osteosarcoma --- lung metastasis --- elisidepsin --- lipid rafts --- hydroxylated lipids --- fatty acid 2-hydroxylase --- cooperative binding --- membrane permeabilization --- marine organisms --- polysaccharides --- anticancer --- anticarcinogenic --- mechanisms of action --- fumigaclavine C --- anti-proliferation --- mitochondrial pathway --- anti-cancer --- anti-proliferative --- carotenoid --- cell cycle arrest --- fucoxanthin --- azoxymethane --- bioactive natural product --- isatin --- in vivo model --- Marthasterias glacialis L. --- palmitic acid --- ER-stress --- CHOP --- Antibody Drug Conjugates (ADCs) --- marine antitumor agents --- clinical trials --- approved antitumor agents --- AD0157 --- angiogenesis --- marine drug --- pyrrolidinedione --- secondary metabolites --- cancer preventive --- chemopreventive --- trabectedin --- plitidepsin --- tumor-associated macrophages --- tumor microenvironment --- preclinical --- anticancer immunity --- antiangiogenesis --- fascaplysin --- cyclin-dependent kinase --- small cell lung cancer --- camptothecin --- poly(ADP-ribose)-polymerase inhibitor --- breast cancer --- seaweed --- therapeutic compounds --- autophagy --- marine drugs --- autophagy inhibitors --- autophagy inducers --- macrolide --- programmed cell death --- energy stress --- araguspongine C --- c-Met --- HER2 --- gemcitabine --- pazopanib --- phase I --- safety --- soft tissue sarcoma --- pachastrissamine --- jaspine B --- carbocyclic analogue --- sphingosine kinase inhibitor --- molecular modeling --- ET-743 --- DNA minor groove binder --- chemotherapy --- bis (2,3-dibromo-4,5-dihydroxy-phenyl)-methane (BDDPM) --- anti-metastatic activity --- cell adhesion --- β1-integrin --- FAK --- BEL-7402 cell --- triterpene glycosides --- sea cucumbers --- antitumor activities --- arrest of cell cycle --- antibacterial --- marangucyclines --- deep-sea --- Streptomyces sp. SCSIO 11594 --- LS-1 --- SNU-C5/5-FU --- TGF-β signaling --- carcinoembryonic antigen --- kalkitoxin --- Moorea producens --- mitochondria toxin --- VEGF --- angiogenesis inhibitor --- hypoxia-inducible factor-1 --- HIF-1 --- Lyngbya majuscula --- marine metabolites --- SZ-685C --- nonfunctioning pituitary adenomas --- Ecklonia cava --- phlorotannins --- dieckol --- migration --- sipholenol A --- ABC transporter --- multidrug resistance --- P-gp/ABCB1 --- BCRP/ABCG2 --- MRP1/ABCC1 --- marine natural products --- glioblastoma --- xyloketal B --- proliferation --- TRPM7 --- marine compound --- ribosomal protein genes --- snoRNA --- FAU --- RPS30 --- SNORA62 --- evolution --- Porifera --- n/a --- Penicillium brevicompactum --- Brevianamide --- Mycochromenic acid derivative --- antifouling --- Caribbean sponge --- plakortide --- endoperoxide --- leukemia --- multi-drug resistant leukemia --- Sarcophyton ehrenbergi --- soft coral --- terpenes --- cembranoids --- cytotoxic activity --- molecular docking --- uveal melanoma --- virtual screening --- Topo I inhibitor --- low toxic --- natural product --- Ulva fasciata --- selenium-containing polysaccharide-protein complex --- pseudopterosin --- NF-κB --- p65 --- inflammation --- cytokine release --- IL-6 --- TNFα --- MCP-1 --- glucocorticoid receptor --- paulomycins --- Micromonospora --- antitumor --- Cantabrian Sea-derived actinobacteria --- puupehenones --- sponges --- antiangiogenic --- antitumoral --- porifera/sponge --- cancer genes --- molecular oncology --- bromophenol --- molecular mechanisms --- cell cycle --- PI3K/Akt --- p38/ERK --- ROS --- human lung cancer --- glycosaminoglycans --- antiproliferative --- heparan sulphate --- gliotoxin --- NSCLC --- adriamycin resistance --- Sepia ink polysaccharides --- antitumour --- chemosensitization --- anticoagulation --- sea anemone --- drug discovery --- endothelial cells --- RGD motif --- kunitz type inhibitor --- prostate cancer --- antioxidant --- natural marine compounds --- marine biotechnology --- microalgae --- marine sponges --- Aeroplysinin --- Isofistularin --- pheochromocytoma and paraganglioma --- metastasis --- cancer progression --- cell adhesion molecules --- integrin β1 --- hypoxia --- phycocyanin --- non-small cell lung cancer --- NF-κB signaling --- marine-derived drugs --- bioanalysis --- chromatography --- manzamine A --- epithelial–mesenchymal transition --- lung cancer --- circulating tumor cells --- signal transduction --- cisplatin --- Lampetra morii --- buccal gland --- cystatin F --- anti-angiogenesis --- cystatin superfamily --- Antimicrobial peptide (AMP) --- Tilapia piscidin 4 (TP4) --- non-small cell lung cancer (NSCLC) --- itampolin A --- FBDD --- p38α --- novel inhibitor --- tetracenomycin X --- cyclin D1 --- proteasomal degradation --- p38 --- c-JUN --- λ-carrageenan --- heparanase --- anticoagulant --- depolymerisation --- cell migration --- Aspergillus --- naphthopyrones --- endophytic fungus --- Leathesia nana --- mangrove-derived actinomycete --- ansamycins --- divergolides --- apoptosis-inducing activity --- actinomycin --- EMT --- invasion --- low molecular weight fucoidan extract --- N-Ras --- neuroblastoma-rat sarcoma --- Cancer --- programmed cell death-ligand 1 --- programmed cell death-ligand 2 --- human sarcoma cell line (HT1080 cells) --- human normal diploid fibroblast (TIG-1 cells) --- chimera --- chemical conjugation --- anticancer agent --- hybridization --- α9-nicotinic acetylcholine receptors (nAChRs) --- breast cancer cells --- αO-conotoxin GeXIVA --- targeted therapy --- gorgonian --- Leptogorgia --- humulane sesquiterpenoids --- anticancer activity --- 12-deacetyl-12-epi-scalaradial --- HeLa cells --- Nur77 --- MAPK/ERK pathway --- Mycalin A --- C15 acetogenins --- synthetic analogues --- antiproliferative activity --- A375 and HeLa cell lines --- polyoxygenated steroids --- sponge --- Haliclona gracilis --- Thalassia testudinum --- thalassiolin B --- polyphenols --- CYP1A1 --- benzo[a]pyrene --- JNK1/2 --- natural products --- synergism --- A549 cells --- cytoskeleton --- P2X7 receptor --- pollution --- anti-angiogenic --- gene expression --- HSP90 --- inhibitor --- epithelial-mesenchymal transition