《Synthesis of indole-based acetohydrazide analogs: their in vitro and in silico thymidine phosphorylase studies》 was written by Taha, Muhammad; Aldhamin, Ebaa Ahmed Jassim; Almandil, Noor Barak; Anouar, El Hassane; Uddin, Nizam; Alomari, Munther; Rahim, Fazal; Adalat, Bushra; Ibrahim, Mohamad; Nawaz, Fasial; Iqbal, Naveed; Alghanem, Bandar; Altolayyan, Abdulelah; Khan, Khalid Mohammed. Category: alcohols-buliding-blocks And the article was included in Bioorganic Chemistry in 2020. The article conveys some information:
In this study, a series of indole-based acetohydrazides I [R = 4-HOC6H4, 2-MeOC6H4 2,3-(HO)2C6H3, 2,4-(MeO)2C6H3, etc.] were synthesized and characterized. The products I were tested for their thymidine phosphorylase inhibitory potential. These derivatives inhibited thymidine phosphorylase at different concentration ranging from 1.10 ± 0.10 to 41.10 ± 1.10μM when compared with the standard 7-deazaxanthine (IC50 value 38.68 ± 1.12μM). The compound I [R = 2,4,6-(HO)3C6H2] was found to be the most potent among the series with IC50 1.10 ± 0.10μM. The structure activity relationships have been established for all compounds keeping in the view the role of substitution and the effect of functional group which significantly affect thymidine phosphorylase activity. The nature of binding interactions of the most potent compounds and active sites of the enzymes was confirmed through mol. docking study. In the experiment, the researchers used 3-Hydroxybenzaldehyde(cas: 100-83-4Category: alcohols-buliding-blocks)
3-Hydroxybenzaldehyde(cas: 100-83-4) can be used as a reactant along with ethyl acetoacetate and thiourea in the synthesis of corresponding dihydropyrimidine-2-thione (monastrol), using Yb(OTf)3 as a catalyst by Biginelli cyclocondensation reaction.Category: alcohols-buliding-blocks
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts