Synthesis and antitumor activity of novel indole derivatives containing α-aminophosphonate moieties
TLDR
A series of novel indole derivatives containing α-aminophosphonate moieties were synthesized as antitumor agents and it is noteworthy that compound B7 displayed higher inhibitory activities against MGC-803 than that of 5-fluorouracil.About:
This article is published in Arabian Journal of Chemistry.The article was published on 2021-08-01 and is currently open access. It has received 13 citations till now. The article focuses on the topics: Aminophosphonate & MTT assay.read more
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Synthesis of Novel Indole Schiff Base Compounds and Their Antifungal Activities
Caixia Wang,Liangxin Fan,Zhenliang Pan,Sufang Fan,Lijun Shi,Xu Li,Jinfang Zhao,Lulu Wu,Guo-Yu Yang,Cuilian Xu +9 more
TL;DR: A series of novel indole Schiff base derivatives (2a–2t) containing a 1,3,4-thiadiazole scaffold modified with a thioether group were synthesized, and their structures were confirmed using FT-IR, 1H N MR, 13C NMR, and HR-MS.
Journal ArticleDOI
New Borane-Protected Derivatives of α-Aminophosphonous Acid as Anti-Osteosarcoma Agents: ADME Analysis and Molecular Modeling, In Vitro Studies on Anti-Cancer Activities, and NEP Inhibition as a Possible Mechanism of Anti-Proliferative Activity
Magdalena Mizerska-Kowalska,Sylwia Sowa,Beata Donarska,Wojciech Plazinski,Adrianna Sławińska-Brych,Aleksandra Tomasik,Anna Ziarkowska,Krzysztof Z. Łączkowski,Barbara Zdzisińska +8 more
TL;DR: Evaluating new borane-protected derivatives of phosphonous acid in terms of their drug-likeness properties, anti-osteosarcoma activities in vitro (against HOS and Saos-2 cells), and use as potential NEP inhibitors shows that compound 4 can be considered a potential anti-stochastic agent and a scaffold for the development of new N EP inhibitors.
Journal ArticleDOI
Synthesis, bioinformatics and biological evaluation of novel α-aminophosphonates as antibacterial agents: DFT, Molecular Docking and ADME/T Studies
Hacène K'tir,Aïcha Amira,Chahrazed Benzaid,Zineb Aouf,Souad Benharoun,Yasmine Chemam,Rachida Zerrouki,Nour-Eddine Aouf +7 more
TL;DR: Novel α-aminophosphonates containing 1,2,3-oxathizolidine-2,2-dioxide moiety have the potential to become lead molecules in the drug discovery process according to the structure-activity relationship study and molecular docking evaluation.
Journal ArticleDOI
Microwave-assisted synthesis of novel sulfonamide-based compounds bearing α-aminophosphonate and their antimicrobial properties
Eman Sabry,Hanan A. Mohamed,Ewies F. Ewies,Benson M. Kariuki,Osama M. Darwesh,Mohamed S. Bekheit +5 more
TL;DR: A series of α-aminophosphonates (3a-3m) bearing the sulfisoxazole moiety was synthesized through one-pot Kabachnik-Fields reaction as mentioned in this paper .
Journal ArticleDOI
Directing group strategies in rhodium-catalyzed C-H amination.
TL;DR: In this paper , the reactivity and selectivity of chelation-assisted rhodium-catalyzed C-H amination are discussed in relation to the types of aminating reagent, as well as the challenges and future development prospects in this field.
References
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Journal ArticleDOI
From nature to drug discovery: the indole scaffold as a 'privileged structure'.
TL;DR: The indole scaffold probably represents one of the most important structural subunits for the discovery of new drug candidates, explaining the great number of drugs that contain the indole substructure, such as indomethacin, ergotamine, frovatriptan, ondansetron, tadalafil, among many others.
Book
Aminophosphonic and aminophosphinic acids : chemistry and biological activity
Harry R. Hudson,Valery Kukhar +1 more
TL;DR: Kudzin et al. as mentioned in this paper proposed an asymmetric synthesis of Aminophosphonates and Aminophophosphinopeptides using side-chain C-P linkages.
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Discovery of Potent Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods and Structure-Based Design
Anders Friberg,Dominico Vigil,Bin Zhao,R. Nathan Daniels,Jason P. Burke,Pedro M. Garcia-Barrantes,DeMarco V. Camper,Brian A. Chauder,Taekyu Lee,Edward T. Olejniczak,Stephen W. Fesik +10 more
TL;DR: The discovery of potent and selective Mcl-1 inhibitors using fragment-based methods and structure-based design and detailed information about the molecular recognition of small-molecule ligands binding M cl-1 is described.
Journal ArticleDOI
Aminophosphonic Acids and Derivatives. Synthesis and Biological Applications
TL;DR: An up-to-date account of the chemistry, the synthesis and the biological activity of aminophosphonic acids and their derivatives is given.
Journal ArticleDOI
Indole: A privileged scaffold for the design of anti-cancer agents.
TL;DR: This review aimed to provide a clear knowledge on the recent development of indoles as anti-cancer agents, such as myeloid cell leukemia-1 (Mcl-1) inhibitors, proviral insertion site in moloney murine leukemia virus (Pim), and made an insight into the corresponding structure-activity relationships (SARs).