2729-19-3Relevant articles and documents
Synthesis of new 2,2-dimethyl-2H-chromen derivatives as potential anticancer agents
Noolvi, M. N.,Patel, Meghna,Patel, Zinal
, p. 874 - 880 (2021/09/28)
The synthesis of some new heterocyclic derivatives comprising imidazothaidiazole, diaryl ketone and chromen as starting compound has been reported. The new series of chromen analogues have been synthesized. The reaction has been monitored by Thin Layer Chromatography (TLC) using suitable mobile phase. The Rf values have been compared and the melting points of derivatives determined. Further, these derivatives have been characterized and confirmed by IR,1H NMR and mass spectral (MS) studies. All the selected compounds submitted to National Cancer Institute (NCI) for in vitro anticancer assay have been evaluated for their anticancer activity.
Synthesis and antiseizure activity of (E)-1,2-diarylethylidenehydrazine carboximidamides against tonic-clonic seizures: an intracerebroventricular and electrophysiological study
Firouzjaei, Fariba Abedi,Heidarli, Elmira,Ravan, Shabnam,Hosseini, Sayed Masoud,Naderi, Nima,Almasyan, Kiarash,Sarvary, Afshin,Irannejad, Hamid
, p. 1520 - 1535 (2020/06/17)
A series of (E)-1,2-diarylethylidenehydrazine carboximidamides 2a–j were synthesized and characterized by NOESY experiment as anticonvulsant agents and their antiseizure activity was evaluated by intracerebroventricular administration of compounds. Most of the compounds had significant protection against tonic-clonic seizures and 2a was found to be as equipotent as carbamazepine in seizures control. In order to find their anticonvulsant mechanism of action, 2a was subjected to further electrophysiological studies using patch-clamp technique. The results confirmed that this compound is neither a voltage-gated sodium channel blocker nor a NMDA/AMPA antagonist. Although 2a did not show any direct GABA agonistic activity, it could decrease EPSP and increase IPSP frequency without any change in amplitude. Finally, the results indicated most likely a presynaptic GABA-mediated mechanism of 2a for its antiseizure activity such as inhibition of the GABA-T which was validated by molecular docking.
Synthesis of substituted phenanthrofurans
Chan, Chieh-Kai,Chen, Yi-Chia,Chen, Yeh-Long,Chang, Meng-Yang
, p. 9187 - 9195 (2015/11/27)
A three-step protocol toward phenanthrofurans 1 starting with deoxybenzoins 3 is developed with moderate to good yield. A facile process is carried out for the (1) α-propargylation of 3 with NaH and propargyl bromide 2 in refluxing THF, (2) Bi(OTf)3-mediated cycloisomerization of γ-ynones 4 with 4 ? molecular sieves in MeNO2 at rt, and (3) photolytic Scholl annulation of 2,3-diarylfurans 5 with I2 in EtOAc at rt. The key structures of 1 are confirmed by X-ray crystallographic analysis.