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Book
Selected Papers from XVI MaNaPro and XI ECMNP
Authors: --- ---
Year: 2021 Publisher: Basel, Switzerland MDPI - Multidisciplinary Digital Publishing Institute

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Abstract

The oceans harbor the majority of the Earth´s biodiversity. Marine organisms/microorganisms provide a diverse array of natural products, which are important sources of biologically active agents with unique chemical structures and a broad range of medical and biotechnological applications. The XVI MaNaPro and XI ECMNP conferences aim to present advances and future perspectives on marine natural product research to the scientific community by gathering scientists who work in marine chemistry and related scientific fields from all over the world and at different seniority levels. This Special Issue was organized on the occasion of the 2nd joint XVI MaNaPro and XI ECMNP meeting (http://wmnp2019.ipleiria.pt/) held in Peniche, Portugal, in 2019. It comprises 12 original research articles that exemplify research performed in the scope of the conference topics

Keywords

marine-derived fungi --- secondary metabolites --- polyketides --- drimanes --- meroterpenoids --- cytotoxicity --- benthic cyanobacteria --- tropical mangrove --- Guadeloupe --- phylogenetic diversity --- chemical diversity --- molecular networking --- antimicrobial activity --- proteasome inhibition --- dolabellane --- secosteroids --- soft coral --- n/a --- marine natural products --- actinomycetes --- biofouling --- antifouling --- antibiofilm --- napyradiomycins --- hybrid isoprenoids --- drug discovery --- bioprospection --- Dysidea avara --- avarone/avarol --- redox-active compounds --- quinones and hydroquinones --- dioxothiazinoquinone --- Schistosoma mansoni --- Plasmodium falciparum --- Leishmania spp. --- 3D-SAR analysis --- DFT studies --- PhenoTarget approach --- MRMS --- protein-ligand complex --- polycarpine --- holothurian --- diatom --- anti-fouling compounds --- saponins --- triterpene glycosides --- mass spectrometry --- Antarctica --- ascidian --- microbiome --- microbial diversity --- palmerolide A --- co-occurrence --- porphyrinoids --- annelida --- marine bioproducts --- HPLC-DAD --- toxicity --- photosensitizers --- chirality --- configurational analysis --- distance geometry --- NMR spectroscopy --- NOE data --- residual dipolar couplings --- Sarcophyton cherbonnieri --- cembranoid --- anti-inflammatory activity --- elastase release --- superoxide anion generation --- osteoarthritis --- amentadione --- preclinical osteoarthritis models --- marine compounds --- Cystoseira usneoides --- inflammation --- mineralization --- chondrocytes --- synoviocytes --- cartilage explants


Book
Advances in Antifungal Development: Discovery of New Drugs and Drug Repurposing
Authors: --- ---
Year: 2022 Publisher: Basel MDPI - Multidisciplinary Digital Publishing Institute

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Abstract

This reprint describes recent advances made in the field of antifungal development, especially the discovery of new drugs and drug repurposing. The articles presented in this book provide useful information and insight for the development of new antifungal drugs or intervention strategies. The identification of new, safe molecules, and cellular targets, as well as the elucidation of their antifungal mechanisms of action, will further the effective control of fungal pathogens, especially those resistant to current therapeutic agents.

Keywords

nanoparticles --- fungi --- drug delivery systems --- marine --- biological synthesis --- myconanotechnology --- canesten --- clotrimazole --- vulvovaginal --- vaginitis --- mycosis --- candidosis --- yeast infection --- candida --- candida albicans --- vaginal health --- anticandidal activity --- indazole --- pyrazole --- 3-phenyl-1H-indazole --- drug design --- acetylsalicylic acid (ASA, aspirin) --- capsule --- CAP64 --- Cryptococcus --- membrane potential (ΔΨM) --- photodynamic treatment --- photosensitiser --- ultrastructure --- drug repurposing --- antifungals --- repositioning --- yeasts --- emerging fungi --- multidrug resistance --- therapeutic alternatives --- new targets --- Candida auris --- Aspergillus spp. --- antifungal --- beta-glucan --- polycations --- Galleria mellonella model --- retinoids --- Candida spp. --- onychomycosis --- Malassezia spp. --- dermatophytes --- microbiology --- mycology --- all-trans retinoic acid --- Acanthamoeba --- free-living ameba --- Acanthamoeba keratitis --- isavuconazonium sulfate --- cyst --- drug --- drug discovery --- drug targets --- invasive aspergillosis treatment --- invasive fungal infections --- fission yeast --- cell wall --- β(1,3)-D-glucan synthase --- antifungal drugs --- echinocandin drugs --- echinocandin resistance --- Fks resistance hot spots --- cytokinesis --- septation --- cell separation --- cell integrity --- cell lysis --- sporotrichosis --- Felis catus --- quinones --- hydrazones --- zoonoses --- host-directed drug therapy --- azoles --- polyenes --- echinocandins --- viral infections --- azole --- synergy --- resistance --- Candida --- natural products --- n/a


Book
Anticancer Agents : Design, Synthesis and Evaluation
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Year: 2021 Publisher: Basel, Switzerland MDPI - Multidisciplinary Digital Publishing Institute

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Abstract

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.

Keywords

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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