3943-74-6Relevant articles and documents
Hydroquinone glycosides from leaves of Myrsine seguinii
Zhong, Xi-Ning,Otsuka, Hideaki,Ide, Toshinori,Hirata, Eiji,Takushi, Anki,Takeda, Yoshio
, p. 2149 - 2153 (1998)
From leaves of Myrsine seguinii, seven hydroquinone glycosides were isolated. By spectroscopic analyses, their structures were elucidated to be arbutin, arbutin 2'- and 6'-O-β-apiofuranosides (seguinosides A and B, respectively), and the benzoyl, p-hydroxybenzoyl, 3-methoxy-4-hydroxybenzoyl and 3,5-dimethoxy-4-hydroxybenzoyl esters of the alcohol hydroxyl group on C- 5'' of arbutin 2'-O-β-apiofuranoside (seguinosides C-F, respectively).
Diploquinones A and B, Two New Phytotoxic Tetrasubstituted 1,4-Naphthoquinones from Diplodia mutila, a Causal Agent of Grapevine Trunk Disease
Reveglia, Pierluigi,Savocchia, Sandra,Billones-Baaijens, Regina,Masi, Marco,Cimmino, Alessio,Evidente, Antonio
, p. 11968 - 11973 (2018)
Two new phytotoxic tetrasubstituted 1,4-naphthoquinones, named diploquinones A and B, were isolated together with vanillic acid from Diplodia mutila (DAR78993), a grapevine pathogen involved in Botryosphaeria dieback in Australia. Diploquinones A and B were characterized as 6,7-dihydroxy-2-methoxy-5-methylnaphthalene-1,4-dione and 3,5,7-trihydroxy-2-methoxynaphthalene-1,4-dione using spectroscopic methods (essentially 1D and 2D 1H and 13C NMR and HR ESIMS). The already known vanillic acid was isolated for the first time as fungal phytotoxin and as metabolite of D. mutila. The three compounds were assayed on detached grapevine leaves (Vitis vinifera cv. Shiraz) at concentrations of 10-3 M and 2.5 × 10-3 M. Vanillic acid showed the highest phytotoxic effect on grapevine leaves irrespective of the tested concentration, while diploquinones A and B showed varying degrees of toxicity.
COMPOSITIONS AND METHODS RELATED TO MOLECULAR CONJUGATION
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Page/Page column 80; 81, (2021/06/11)
The invention relates to activated Michael acceptor (AMA) compounds that can undergo conjugation with biomolecules containing Michael donor moieties, thereby providing plasma-stable antibody-drug conjugates (ADCs). Pharmaceutical compositions of the ADCs are disclosed as well. Also provided herein are a number of applications (e.g., therapeutic applications) in which the compositions are useful.
Novel 4-Anilinoquinazoline Derivatives as Potent Anticancer Agents: Design, Synthesis, Cytotoxic Activity, and Docking Study
Dabirian, Sara,Dogaheh, Mahtab Ghasemi,Ghasemi, Saeed,Moghadam, Fatemeh Azmian,Mojabi, Mohammad,Yousefbeyk, Fatemeh
, p. 730 - 739 (2021/10/29)
The simultaneous inhibition of EGFR and VEGFR-2 is a promising method in cancer treatment. In the present work, several 4-Anilinoquinazoline derivatives encompassing different substitutions at the C-4 and C-7 positions of a quinazoline core were designed, synthesised, and evaluated for their cytotoxicity on A431, HUVEC, and HU02 cell lines. Docking studies were carried out to test the interactions of all synthesised compounds with EGFR and VEGFR-2. Furthermore, a wound healing assay was done for the investigation of cell migration. The most potent compound was 8l followed by the compounds 8i and 8j which showed better cytotoxic activities on A431 and HUVEC cell lines than the standard (Vandetanib). The compounds 8f and 8a represented the best docking energies of 8.99 and 9.35 kcal mol-1 for EGFR and VEGFR, respectively. Moreover, molecular docking studies exhibited that compound 8l showed efficient binding affinity against both EGFR and VEGFR-2. It can bind to these receptors through the formation of essential hydrogen bonds between the quinazoline N1 atom and the Met796 backbone of EGFR and two hydrogen bonds with Cys919 and Thr916 of VEGFR-2 with energies of-7.99 and-7.85 kcal mol-1, respectively. In addition, this compound displayed the highest activity on cell migration and wound healing. Compound 8l with the highest cytotoxic activity can be considered a candidate for further investigation and structural optimisation as an antiproliferative agent.