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For this Special Issue book, ten papers focusing on novel bioactive molecules from different marine microorganisms, including fungi, cyanobacteria, actinobacteria and diatoms, were selected. The isolated biomolecules represent different structures and showed anticancer, antiviral, antifungal, antibacterial, anti-inflammatory and enzyme-inhibiting activities. One of the papers is a review article on microviridins, a class of bioactive cyanobacterial peptides.

Medicine --- marine-derived fungus --- Aspergillus terreus --- thiodiketopiperazines --- dihydroisocoumarins --- Epicoccum nigrum --- deep-sea-derived fungus --- diketopiperazine enantiomers --- cytotocxic activity --- diatoms --- marine biotechnology --- anti-inflammatory --- drug discovery --- Cylindrotheca closterium --- mangrove Streptomyces --- genetic dereplication --- anti-microbial --- antiproliferative --- endophyte fungus --- Aspergillus versicolor --- diketopiperazines --- ECD calculation --- enantiomers --- bianthraquinones --- meroterpenoids --- anti-inflammatory activity --- Stemphylium sp. --- cyanobacteria --- nostocyclopeptides --- Nostoc --- ncp gene cluster --- nonribosomal peptide synthetase --- aeruginosamides --- Limnoraphis --- cytotoxicity --- oligopeptide --- microviridin --- biotechnology --- ecology --- Penicillium citrinum --- chromone derivatives --- anti-cancer activity

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The marine environment is considered one of the most important sources of natural bioactive compounds with extremely rich biodiversity. Marine glycans are remarkable molecules, playing a determinant role in biological processes. Marine сarbohydrate-containing substances have drawn increasing attention in the field of biomedicine for their various biological activities, such as antitumor, antivirus, hypoglycemic, immunomodulatory, and anticoagulant. These compounds obtained from marine sources, such as algae, microbes, and animals, are usually biodegradable and biocompatible, and exhibit biological properties that contribute to the discovery of a wide range of new bioactive substances with special pharmacological properties of interest to medicine. Carbohydrate-based compounds include glycans, glycoproteins, proteoglycans, glycolipids, and low-molecular and complex glycosides of differential origin. Many of the polysaccharides allow for loading lower drug dosages, which may lead to a drastic reduction of the side effects caused by the drugs. In addition, the structure of polysaccharides can be relatively easily modified in order to synthesize derivatives with desirable characteristics for drug delivery. Complexes on the basis of carbohydrates are often prepared to improve their functional properties. In this Special Issue, we seek to contribute to the discussion of various aspects of marine carbohydrate-containing compounds and provide a unique platform for a new concept for their use in medicine in order to continue to facilitate further research in this area.

Medicine --- chitosan-gentamicin conjugate --- antimicrobial --- anti-inflammatory --- scald repair --- sulfated polysaccharides --- galactans --- green seaweed --- NMR --- immunostimulation --- inflammatory mediators --- carrageenan --- lipopolysaccharide --- macromolecular structure --- nonspecific resistance to lipopolysaccharide --- cytokines --- enteric infections --- salmonellosis --- glyceroglycolipid metabolism --- phosphate starvation --- transcriptome --- glyceroglycolipid homeostasis --- chitosan --- polyelectrolyte complex --- cytokine --- nitric oxide --- anti-inflammatory activity --- Ulva pertusa --- polysaccharides --- colitis --- antioxidant --- exopolysaccharide --- structure --- Vibrio alginolyticus --- Epidermist --- chitosan oligosaccharides --- inflammation cytokines --- intestine --- oxidative status --- oxidative stress --- Porphyridium marinum --- high pressure homogenizer --- antibacterial activity --- anti-biofilm activity --- anti-cancer activity --- alginate lyase --- cold-adapted --- exo/endo-type --- Alteromonas portus --- oligosaccharide --- antioxidant activity --- exopolysaccharides --- scandium --- theranostic --- cancer cell lines --- proliferation --- laminarin --- fucoidan --- gastrointestinal tract --- microbiome --- swine --- post-weaning --- antibiotic alternatives --- n/a

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The marine environment is considered one of the most important sources of natural bioactive compounds with extremely rich biodiversity. Marine glycans are remarkable molecules, playing a determinant role in biological processes. Marine сarbohydrate-containing substances have drawn increasing attention in the field of biomedicine for their various biological activities, such as antitumor, antivirus, hypoglycemic, immunomodulatory, and anticoagulant. These compounds obtained from marine sources, such as algae, microbes, and animals, are usually biodegradable and biocompatible, and exhibit biological properties that contribute to the discovery of a wide range of new bioactive substances with special pharmacological properties of interest to medicine. Carbohydrate-based compounds include glycans, glycoproteins, proteoglycans, glycolipids, and low-molecular and complex glycosides of differential origin. Many of the polysaccharides allow for loading lower drug dosages, which may lead to a drastic reduction of the side effects caused by the drugs. In addition, the structure of polysaccharides can be relatively easily modified in order to synthesize derivatives with desirable characteristics for drug delivery. Complexes on the basis of carbohydrates are often prepared to improve their functional properties. In this Special Issue, we seek to contribute to the discussion of various aspects of marine carbohydrate-containing compounds and provide a unique platform for a new concept for their use in medicine in order to continue to facilitate further research in this area.

chitosan-gentamicin conjugate --- antimicrobial --- anti-inflammatory --- scald repair --- sulfated polysaccharides --- galactans --- green seaweed --- NMR --- immunostimulation --- inflammatory mediators --- carrageenan --- lipopolysaccharide --- macromolecular structure --- nonspecific resistance to lipopolysaccharide --- cytokines --- enteric infections --- salmonellosis --- glyceroglycolipid metabolism --- phosphate starvation --- transcriptome --- glyceroglycolipid homeostasis --- chitosan --- polyelectrolyte complex --- cytokine --- nitric oxide --- anti-inflammatory activity --- Ulva pertusa --- polysaccharides --- colitis --- antioxidant --- exopolysaccharide --- structure --- Vibrio alginolyticus --- Epidermist --- chitosan oligosaccharides --- inflammation cytokines --- intestine --- oxidative status --- oxidative stress --- Porphyridium marinum --- high pressure homogenizer --- antibacterial activity --- anti-biofilm activity --- anti-cancer activity --- alginate lyase --- cold-adapted --- exo/endo-type --- Alteromonas portus --- oligosaccharide --- antioxidant activity --- exopolysaccharides --- scandium --- theranostic --- cancer cell lines --- proliferation --- laminarin --- fucoidan --- gastrointestinal tract --- microbiome --- swine --- post-weaning --- antibiotic alternatives --- n/a

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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.

Medicine --- 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

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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.

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