Application of 1877-71-0On September 15, 2019 ,《Targeting dihydrofolate reductase: Design, synthesis and biological evaluation of novel 6-substituted pyrrolo[2,3-d]pyrimidines as nonclassical antifolates and as potential antitumor agents》 was published in European Journal of Medicinal Chemistry. The article was written by Gao, Tianfeng; Zhang, Congying; Shi, Xiaowei; Guo, Ran; Zhang, Kai; Gu, Jianmin; Li, Lin; Li, Shuolei; Zheng, Qianqian; Cui, Mengyu; Cui, Miao; Gao, Xingmei; Liu, Yi; Wang, Lei. The article contains the following contents:
A novel series of 6-substituted pyrrolo[2,3-d]pyrimidines with reversed amide moieties from the lead compound I (R = 4-pyridyl) were designed and synthesized as nonclassical antifolates and as potential antitumor agents. Target compounds II were successfully obtained through two sequential condensation reactions from the key intermediate 2-amino-6-(2-aminoethyl)-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidin-4-one. In preliminary antiproliferation assay, all compounds demonstrated submicromolar to nanomolar inhibitory effects against KB tumor cells, whereas compounds I (R = 2-, 3-, 4-pyridyl) also exhibited nanomolar antiproliferative activities toward SW620 and A549 cells. In particular, compounds I (R = 2-, 3-, 4-pyridyl) were significantly more potent than the pos. control methotrexate (MTX) and pemetrexed (PMX) to A549 cells. The growth inhibition induced cell cycle arrest at G1-phase with S-phase suppression. Along with the results of nucleoside protection assays, inhibition assays of dihydrofolate reductase (DHFR) clearly elucidated that the intracellular target of the designed compounds was DHFR. Mol. modeling studies suggested two binding modes of the target compounds with DHFR. In the part of experimental materials, we found many familiar compounds, such as 3-(Methoxycarbonyl)benzoic acid(cas: 1877-71-0Application of 1877-71-0)
3-(Methoxycarbonyl)benzoic acid(cas: 1877-71-0) belongs to esters. They are important in biology, being one of the main classes of lipids and comprising the bulk of animal fats and vegetable oils.Application of 1877-71-0 They perform as high-grade solvents for a broad array of plastics, plasticizers, resins, and lacquers, and are one of the largest classes of synthetic lubricants on the commercial market.
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics