75823-30-2Relevant academic research and scientific papers
Design, synthesis, anticancer evaluation and molecular docking study of novel 2,4-dichlorophenoxymethyl-based derivatives linked to nitrogenous heterocyclic ring systems as potential CDK-2 inhibitors
Almehizia, Abdulrahman A.,Amr, Abd El-Galil E.,El-Sayed, Amira A.,Nossier, Eman S.
, (2021/08/23)
A novel series of 2,4-dichlorophenoxymethyl-based derivatives 4-18 bearing various nitrogenous heterocyclic systems have been designed and synthesized through molecular hybridization approach. The anti-proliferative activity of all newly synthesized derivatives was established against human HCT-116 and MCF-7 cancer cell lines. The structure–activity relationship (SAR) studies exhibited that the derivatives incorporated with pyrido[3,2-d]pyrimidine, naphtho[2,3-e][1,3]oxazine-5-sulfonic acid, benzo[d]thiazole and benzo[d]oxazole scaffolds revealed the highest cytotoxic activities comparing with doxorubicin as a reference drug. The promising derivatives 5, 9, 13 and 15 were subjected to enzymatic inhibitory assessment against CDK-2/cyclin A2 using roscovitine as a standard. Concerning their effects upon the apoptotic process, they upregulated Bax, p-53 and caspase-3 levels and downregulated Bcl-2, causing induction of apoptosis. Moreover, the in silico molecular docking was applied to investigate the possible binding modes and orientations within the active site of CDK-2.
Direct and facile synthesis of acyl isothiocyanates from carboxylic acids using trichloroisocyanuric acid/triphenylphosphine system
Entezari, Najmeh,Akhlaghinia, Batool,Rouhi-Saadabad, Hamed
, p. 201 - 206 (2015/02/05)
A mild, efficient, and practical method for one-step synthesis of alkanoyl and aroyl isothiocyanates from carboxylic acids using a safe and inexpensive mixed reagent, trichloroisocyanuric acid/triphenyl-phosphine is described at room temperature. Availability of the reagents and easy workup of the reaction make this method attractive for organic chemists.
Synthesis and fungicidal activities of some 2-aryloxymethyl-1,3,4-thiadiazolo-quinazolin-4-ones and 2-aryloxymethyl-5-substituted-1,3,4-thiadiazolo-1,3,5-triazine-7-thiones
Tiwari, Nirupama,Chaturvedi, Bandana,Nizamuddin
, p. 200 - 202 (2007/10/02)
Several 2-aryloxymethyl-1,3,4-thiadiazolo-quinazolin-4-ones (Va-e) and 2-aryloxymethyl-5-substituted-1,3,4-thiadiazolo-1,3,5-triazine-7-thiones (IIIa-e) have been synthesized and screened for their antifungal activity against Aspergillus niger and Helminthosporium oryzae.
