934022-19-2Relevant academic research and scientific papers
Antifungal activity of chalcones: A mechanistic study using various yeast strains
Lahtchev,Batovska,Parushev,Ubiyvovk,Sibirny
, p. 2220 - 2228 (2008)
We reported the synthesis, antifungal evaluation and study on substituent effects of 21 chalcones. A lot of genetically defined strains belonging to different yeast genera and species, namely Saccharomyces cerevisiae, Hansenula polymorpha and Kluyveromyces lactis, were used as test organisms. Concerning the mode of the antifungal action of chalcones it was shown that DNA was probably not the main target for the chalcones. It was revealed that the yeast's intracellular glutathione and cysteine molecules play significant role as defence barrier against the chalcone action. It was also shown that chalcones may react with some proteins involved in cell separation.
Novel hybrids derived from aspirin and chalcones potently suppress colorectal cancer in vitro and in vivo
Lu, Shan,Obianom, Obinna N.,Ai, Yong
, p. 1722 - 1732 (2018/10/26)
Colorectal cancer (CRC) remains the fourth leading cause of cancer deaths around the world despite the availability of many approved small molecules for treatment. The issues lie in the potency, selectivity and targeting of these compounds. Therefore, new
Study on the substituents' effects of a series of synthetic chalcones against the yeast Candida albicans
Batovska,Parushev,Slavova,Bankova,Tsvetkova,Ninova,Najdenski
, p. 87 - 92 (2007/10/03)
A large series of chalcones were synthesized and studied for activity against Candida albicans. The SAR analysis showed that the antifungal activity was highly dependent on the substitution pattern of the aryl rings and correlated to a large extent with the ability of compounds to interact with sulfhydryl groups. The most active were the hydroxylated chalcones as their activity related to the location of the phenolic group in the aryl ring B as follows: o-OH > p-OH ～ 3,4-di-OH > m-OH. These and other correlations obtained strongly contribute to the knowledge for design of anticandidal chalcones.
Facile synthesis of aryl-substituted 1,2,5,6-tetrahydropyrimidines and their stereochemical investigation
Chebanov, Valentin A.,Muravyova, Elena A.,Sadchikova, Yulia V.,Desenko, Sergey M.,Chernenko, Vitaly N.,Kobzar, Kiril M.,Musatov, Vladimir I.
, p. 897 - 904 (2007/10/03)
The present work is devoted to the investigation of 2,4,6-triaryl-1,2,5,6- tetrahydropyrimidine derivatives. A new facile approach to their synthesis based on the reaction of α,β-unsaturated ketones, carbonyl compounds and ammonia was developed. Some stereochemical features of the compounds obtained were fixed on the base of NMR data (including COSY and NOESY experiments).
