2 edition of synthesis and antitumour evaluation of methylamino compounds. found in the catalog.
synthesis and antitumour evaluation of methylamino compounds.
Simon Peter Langdon
Thesis (PhD) - University of Aston in Birmingham, 1983.
(). Synthesis and Biological Evaluation of Novel Phosphonates Derivatives of As Potential Antitumor Agents. Phosphorus, Sulfur, and Silicon and the . The synthesis of 4-methoxycarbonylmethylisoquinolinequinone (1) and a variety of its substitution products with amino-, alkylamino and halogen groups on the quinone nucleus is reported. The series of 6-, 7- and 6,7-subtituted isoquinolinequinones were evaluated in vitro for their cytotoxic activity using the MTT colorimetric method. All the newly synthesized compounds showed moderate to.
Title:Synthesis and Antitumor Activity of New Pyrimidine and Caffeine Derivatives VOLUME: 12 ISSUE: 6 Author(s):Ameen Ali Abu-Hashem and Hoda Abdel Raouf Hussein Affiliation:Photochemistry Department (Heterocyclic Unit), National Research Center, , Dokki, Giza, Egypt and b Department of Chemistry, Faculty of Science, Jazan University, Jazan, Saudi Arabia. A series of N-arylaryl-pyrazolo[1,5-a]pyrimidines 18a–u and N-aryl-pyrazolo[1,5-a]quinazolines 25a–c were designed and synthesized via the reaction of 5-aminopyrazoles 11a–c with enaminones 12a–g or 19, respectively. The new compounds were screened for their in vitro antitumor activity toward liver (HepG-2) and breast (MCF-7) human cancer cells using 3-[4,5-dimethylthiazolyl)-2,5.
The first asymmetric total synthesis of ophiorrhisine A (1), a new cyclic tetrapeptide isolated from Ophiorrhiza nutans, was accomplished via an intramolecular aromatic nucleophilic substitution reaction (IMSNAr) of a linear tripeptide to construct a membered paracyclophane ring, resulting in confirmation of its structure and absolute configuration. The structure–activity relationship. A series of novel hydroxyprotopanaxadiol (OH-PPD) derivatives were synthesized by reacting with amino acids, and their in vitro antitumor activities were evaluated on five human tumor cell lines. According to the bioassay results, compounds 3xt and 9xt displayed the most potent anticancer activities with IC 50 values ranging from to μM and – μM, respectively.
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3. Cytotoxic evaluation. The antitumor activities in vitro of these compounds were evaluated by sulforhodamine B (SRB) assay 11 against A (human lung cancer cell) and MTT tetrazolium dye assay 12 against P (murine leukemia cell), respectively.
The IC 50 represents the drug concentration (micromolar) required to inhibit cell growth by 50%.Cited by: The synthesis and antitumour evaluation of methylamino compounds Author: Langdon, Simon : Simon P. Langdon. Synthesis and Antitumor Activity Evaluation of Compounds Based on Toluquinol by Iván Cheng-Sánchez 1,†, José A.
Torres-Vargas 2,3,†, Beatriz Martínez-Poveda 2,3, Guillermo A. Guerrero-Vásquez 1, Miguel Ángel Medina 2,3,4, Francisco Sarabia 1,* and Ana R. Quesada 2,3,4,*Cited by: 1. Introduction.
In recent years, interest in the chemistry of hydrazonoyl halides has been renewed because of the development of novel synthetic routes and their use as synthons for compounds that find many applications [1,2,3,4,5,6,7,8,9,10].The literature reveals that the presence of a morpholine ring on a heterocyclic system contributes to enhanced pharmacological activities in many cases.
Title:Synthesis and Evaluation of Novel Erucin Analogues as Potential Antitumor Compounds VOLUME: 15 ISSUE: 3 Author(s):Yan-Dong Shao, Huang-Wang Song, Wen Feng, Xiang-Hui Wang*, Zai-Feng Shi, Lu-Yong Wu, Guang-Ying Chen and Qiang Lin* Affiliation:Key Laboratory of Water Pollution Treatment and Resource Reuse of Hainan Province, Hainan Normal University, Haikou.
Compound 25 exhibited the similar anti-tumor efficacy with epacadostat without inducing significant change in body weight compared to the control group.
Abstract Indoleamine 2,3-dioxygenase 1 (IDO1) is the enzyme catalyzing the oxidative metabolism of tryptophan, which accounts for cancer immunosuppression in tumor microenvironment.
The percentage of cell survival was calculated as OD value of cells treated with test compound − OD value of culture medium/(OD value of control cells − OD value of culture medium) × % and IC 50 was calculated as the concentration which resulted in 50% of cell death.
In vivo anti-tumor activity. Kunming mice were used. A series of novel N-aryl(benzo[d][1,3]dioxolylmethyl)(tert-butyl)thiazolamines (C1–C31) were synthesized and evaluated for their antitumor activities against HeLa, A and MCF-7 cell tested compounds showed potent growth inhibition properties with IC 50 values generally below 5 μM against the three human cancer cells by: 6.
Compound 1 was derived from selenium by sodium borohydride reduction in the presence of ethanol under nitrogen atmosphere. The reaction of benzonitrile(2) with sodium hydrogen selenide(1) yielded selenobenzamide 3, which was reacted with 1,3-dichloroacetone in acetone to produce compound 4 at room temperature for 4 nd 5 was made by the reaction of 4 and 2.
Title:Synthesis and Antitumor Invasive Activity of Novel Ionone Alkaloid Derivatives VOLUME: 11 ISSUE: 4 Author(s):Hai-Jun Fang, Qian Liu, Chun-Chun Gan, Mei-Na Jin, Nan Qin and Hong-Quan Duan Affiliation:Research Center of Basic Medical Sciences, Tianjin Medical University, TianjinPeople's Republic of China.
Keywords:Antitumor metastasis, Breast cancer cells, Derivative synthesis. Biological evaluation Antimicrobial and antiquorum-sensing evaluation. Compounds 3a-p were estimated for in vitro antimicrobial efficacy toward Gram -ve bacterium (Escherichia coli), Gram + ve bacteria (Bacillus cereus and Staphylococcus aureus) and pathogenic fungi (Candida albicans and Aspergillus fumigatus ) using amoxicillin as a standard antibacterial.
Design, synthesis, and antitumor evaluation of histone deacetylase inhibitors with l-phenylglycine scaffold. Yingjie Zhang, 1 Xiaoguang Li, 1 Jinning Hou, 1 Yongxue Huang, 2 and Wenfang Xu 1 All the obtained data were used to evaluate the antitumor potency and toxicity of compounds.
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We also acknowledge previous National Science Foundation support under grant numbers. Synthesis strat egies of, -thiazole deriv atives Thiazole ring syst em w ere easily synthesiz ed by w ell-kno wn methods o f Hantzsch [ 22 ], Cook- Heilbron [ 23 ], and Gabriel [ 24 ].
These compounds used sorafenib as the lead compound and achieved modifications using bioisosteres and the alkyl principle. The in vitro the results showed that compounds 3c, 3d, 3h, 3n, 3r, and 3z had good inhibitory effects on human cervical cancer cells (Hela), while compounds 3t and 3v had good inhibitory effects on human lung cancer.
In this report, we describe the synthesis and biologic properties of compounds 1–3, analogs of compound 4 with 1 to 3 bridge carbons, respectively, linking a 6-substituted pyrrolo[2,3-d]pyrimidine moiety with a thienoyl ring, for direct comparison with compound results demonstrate the dramatically increased potency of compound 3 toward both PCFT- and FR-expressing cells.
Furthermore, the docking result of compound 2 with EGFR TM (PDB ID code: 3IKA) exhibited that except the covalent bond with CYS and other two hydrogen bond with MET (same to osimertinib, Fig. S1A), compound 2 could form a new salt bridge with LYS, which may be another reason for its good antitumor efficacy in vivo.
Coibamide A has eight N-methylamino acids and two ester coupling of an amino acid onto the N-methylamino terminus of a peptidyl resin proceeds slowly because of steric hindrance, and the synthesis of N-methyl-rich peptides can be made difficult by the sluggish nature of this reaction. 4 The synthesis of N-methyl-rich peptides on a solid-support therefore requires the.
An asymmetric synthesis of a series of novel 4-methyl-(3'S,4'S)-cis-khellactone derivatives 3a–o is reported for the first time. Their structures were confirmed by 1H-NMR, 13C-NMR and MS. Their cytotoxic activity was evaluated by the MTT assay against three selected human cancer cell lines: HEPG-2 (human liver carcinoma), SGC (human gastric carcinoma), LST (human colon carcinoma).
Aziridine-containing compounds have been of interest as anticancer agents since late s. The design, synthesis and study of triaziquone (TZQ) analogues with the aim of obtaining compounds with enhanced efficacy and reduced toxicity are an ongoing research effort in our group.
A series of bis-type TZQ derivatives has been prepared and their cytotoxic activities were investigated. Design, Synthesis, and Pharmacological Evaluation of Novel Hybrid Compounds to Treat Sickle Cell Disease Symptoms.
Part II: Furoxan Derivatives. Journal of Medicinal Chemistry55 (17), DOI: /jmn.2-Aminomethylbenzothiazole (II) Fifteen milliliters of concentrated H 2 SO 4 was added to p-tolylthiourea ( g) and the temperature of the mixture was raised to 80°C on a water bath.
Next, 48% HBr ( g) acid was added slowly and the reaction mixture was stirred for two hours and set at 80°C.A series of polyhalo acridone heterocyclic compounds were synthesized and evaluated for their in vitro antitumor activity.
It was noteworthy that halogen atoms were present at the 1, 3 and 4 sites of the compounds, and an amide group or a cyano group was at the 2 site. The antitumor bioactivity screening revealed t.