- Synthesis of flavone derivatives via N-amination and evaluation of their anticancer activities
-
Seventeen new flavone derivatives substituted at the 40-OH position were designed, synthesized and evaluated for their anticancer and antibacterial activities. Among them, compounds 3, 4, 6f, 6e, 6b, 6c and 6k demonstrated the most potent antiproliferative activities against a human erythroleukemia cell line (HEL) and a prostate cancer cell line (PC3). The results also showed that the IC50 value of compounds 3, 4, 6f, 6e, 6b, 6c and 6k were close to that of the anticancer drug cisplatin (DDP) and lower than that of apigenin. All of the derivatives did not present antibacterial activities. The structure–activity relationships evaluation showed that the configuration of methyl amino acid might affect their biological activities.
- Zhang, Ni,Yang, Jin,Li, Ke,Luo, Jun,Yang, Su,Song, Jun-Rong,Chen, Chao,Pan, Wei-Dong
-
-
Read Online
- Flavonoid derivative with tumor cell inhibition and preparation method and application thereof
-
The invention relates to a flavonoid derivative and a preparation method and application thereof. A coupling reaction is used to prepare the flavonoid derivative, 4'-OH is replaced with an amino substituted substance, and a nitrogen-containing derivative is synthesized on a flavonoid skeleton. By introducing the amino substituted substance, hydrogen bonding of the flavonoid derivative and a target protein can be regulated, and at the same time, an ester water partition coefficient can be also regulated, so that the flavonoid derivative can pass a blood-brain barrier relatively well, and thereby plays a role in inhibiting tumor cells. An anti-proliferative activity research of the flavonoid derivative in tumor cells HEL and PC3 is studied by MTT assay, results show that the flavonoid derivative has good anti-proliferative activity against the tumor cells HEL and PC3, and has higher antitumor activity than natural flavonoid apigenin, and the anti-proliferative effect of the flavonoid derivative is similar to that of clinical anti-tumor drug cisplatin.
- -
-
Paragraph 0016; 0018
(2019/10/01)
-
- Structure-Activity Relationships of cyclo(l -Tyrosyl- l -tyrosine) Derivatives Binding to Mycobacterium tuberculosis CYP121: Iodinated Analogues Promote Shift to High-Spin Adduct
-
A series of analogues of cyclo(l-tyrosyl-l-tyrosine), the substrate of the Mycobacterium tuberculosis enzyme CYP121, have been synthesized and analyzed by UV-vis and electron paramagnetic resonance spectroscopy and by X-ray crystallography. The introduction of iodine substituents onto cyclo(l-tyrosyl-l-tyrosine) results in sub-μM binding affinity for the CYP121 enzyme and a complete shift to the high-spin state of the heme FeIII. The introduction of halogens that are able to interact with heme groups is thus a feasible approach to the development of next-generation, tight binding inhibitors of the CYP121 enzyme, in the search for novel antitubercular compounds.
- Rajput, Sunnia,McLean, Kirsty J.,Poddar, Harshwardhan,Selvam, Irwin R.,Nagalingam, Gayathri,Triccas, James A.,Levy, Colin W.,Munro, Andrew W.,Hutton, Craig A.
-
supporting information
p. 9792 - 9805
(2019/11/13)
-
- Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitor Agents: Optimization of Diarylanilines with High Potency against Wild-Type and Rilpivirine-Resistant E138K Mutant Virus
-
Three series (6, 13, and 14) of new diarylaniline (DAAN) analogues were designed, synthesized, and evaluated for anti-HIV potency, especially against the E138K viral strain with a major mutation conferring resistance to the new-generation non-nucleoside reverse transcriptase inhibitor drug rilpivirine (1b). Promising new compounds were then assessed for physicochemical and associated pharmaceutical properties, including aqueous solubility, log P value, and metabolic stability, as well as predicted lipophilic parameters of ligand efficiency, ligand lipophilic efficiency, and ligand efficiency-dependent lipophilicity indices, which are associated with ADME property profiles. Compounds 6a, 14c, and 14d showed high potency against the 1b-resistant E138K mutated viral strain as well as good balance between anti-HIV-1 activity and desirable druglike properties. From the perspective of optimizing future NNRTI compounds as clinical trial candidates, computational modeling results provided valuable information about how the R1 group might provide greater efficacy against the E138K mutant.
- Liu, Na,Wei, Lei,Huang, Li,Yu, Fei,Zheng, Weifan,Qin, Bingjie,Zhu, Dong-Qin,Morris-Natschke, Susan L.,Jiang, Shibo,Chen, Chin-Ho,Lee, Kuo-Hsiung,Xie, Lan
-
p. 3689 - 3704
(2016/05/24)
-
- TREATMENT OF DISEASES BY EPIGENETIC REGULATION
-
The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. The disclosed compositions and methods can be used for treatment and prevention of diseases or disorders that are susceptible to administration of a BET inhibitor.
- -
-
Paragraph 0372; 0373
(2013/11/05)
-
- Electronic-state switching strategy in the photochemical synthesis of indanones from o-methyl phenacyl epoxides
-
An electronic excited-state switching strategy has been utilized to control the selectivity of a key photochemical step in the total synthesis of indanorine. The excited-state character of 4, 5-dimethoxy-2-methylphenacyl epoxide was changed from an unfavorable 3φ , φ * state to a productive 3n, φ * state by a temporary structural modification, resulting in a relatively efficient and high-yielding formation of an indanone derivative. The corresponding structural modification was selected on the basis of quantum chemical calculations prior to the synthesis.
- Stacko, Peter,Solomek, Tomas,Klan, Petr
-
p. 6556 - 6559
(2012/02/15)
-
- Biological evaluation of KRIBB3 analogs as a microtubule polymerization inhibitor
-
A series of KRIBB3 analogs were synthesized by modifying substituents at aryl moieties of KRIBB3 for examining structure-activity relationships, and their inhibitory activities on microtubule polymerization were evaluated. The presence of free phenolic hydrogens in aryl moieties of KRIBB3 analogs plays an important role in inhibition of microtubule polymerization.
- Lee, Sangku,Kim, Jae Nyoung,Lee, Hyeong Kyu,Yoon, Kab Seog,Shin, Ki Deok,Kwon, Byoung-Mog,Han, Dong Cho
-
experimental part
p. 977 - 979
(2011/03/21)
-
- NOVEL ANTI-INFLAMMATORY AGENTS
-
Disclosed are methods of regulating interleukin-6 (IL-6) and/or vascular cell adhesion molecule-1 (VCAM-1) and methods of treating and/or preventing cardiovascular and inflammatory diseases and related disease states, such as, for example, atherosclerosis, asthma, arthritis, cancer, multiple sclerosis, psoriasis, and inflammatory bowel diseases, and autoimmune disease(s) by administering a naturally occurring or synthetic quinazolone derivative. The invention provides novel synthetic quinazolone compounds, as well as pharmaceutical compositions comprising those compounds.
- -
-
Page/Page column 57-59
(2010/11/05)
-
- Substituted compounds derived from N-(benzyl)phenylacetamide, preparation and uses
-
This invention relates to poly-substituted derivatives of the N-(benzyl)phenylacetamide type, pharmaceutical compositions comprising same, therapeutic uses thereof, more particularly in the fields of human and animal health. This invention also relates to a process for the preparation of such derivatives.
- -
-
Page/Page column 45
(2010/10/20)
-
- CGRP ANTAGONISTS, METHOD FOR THE PRODUCTION THEREOF, AND THEIR USE AS MEDICAMENTS
-
The invention relates to CGRP antagonists of general formula (I) in which: R1, R2, R3, R4 and X are defined as in Claim 1, to their tautomers, isomers, diastereomers, enantiomers, hydrates, mixtures and salts as well as the hydrates of the salts, in particular, their physiologically compatible salts with inorganic or organic acids and bases, and those compounds of general formula (I) in which one or more hydrogen atoms are replaced by deuterium. The invention also relates to medicaments containing these compounds, the use thereof, and to methods for producing them.
- -
-
Page/Page column 142-143
(2008/06/13)
-
- 4-oxy-substituted phenoxyalkyl carboxylic acid, ester, and alcohol derivatives as antihyper-cholesterolemic and antiatherosclerotic agents
-
Novel 4-oxy substituted phenoxyalkyl carboxylic acid, ester and alcohol derivatives are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful in preventing the intestinal absorption of cholesterol and thus are useful in the treatment of hypercholesterolemia and atherosclerosis.
- -
-
-