58654-89-0Relevant academic research and scientific papers
Design, synthesis and biological evaluation of novel 2,4-disubstituted quinazoline derivatives targeting H1975 cells via EGFR-PI3K signaling pathway
Chao, Gao,Dai, Honglin,Ke, Yu,Li, Erdong,Lihong, Shan,Liu, Hongmin,Liu, Limin,Si, Xiaojie,Wang, Zhengjie,Yang, Zhang,Zhang, Luye,Zhang, Qiurong,Zheng, Jiaxin
, (2021/07/28)
In order to find new and highly effective anti-tumor drugs with targeted therapeutic effects, a series of novel 4-aminoquinazoline derivatives containing N-phenylacetamide structure were designed, synthesized and evaluated for antitumor activity against four human cancer cell lines (H1975, PC-3, MDA-MB-231 and MGC-803) using MTT assay. The results showed that the compound 19e had the most potent antiproliferative activity against H1975, PC-3, MDA-MB-231 and MGC-803 cell lines. At the same time, compound 19e could significantly inhibit the colony formation and migration of H1975 cells. Compound 19e also arrested the H1975 cell cycle in the G1 phase and mediated cell apoptosis, promoted the accumulation of ROS in H1975 cells. Furthermore, compound 19e exerted antitumor effect in vitro by reducing the expression of anti-apoptotic protein Bcl-2 and increasing the pro-apoptotic protein Bax and p53. Mechanistically, compound 19e could significantly decreased the phosphorylation of EGFR and its downstream protein PI3K in H1975 cells. Which indicated that compound 19e targeted H1975 cell via interfering with EGFR-PI3K signaling pathway. Molecular docking showed that compound 19e could bind into the active pocket of EGFR. Those work suggested that compound 19e would have remarkable implications for further design of anti-tumor agents.
Slight structural modulation around a pivotal bond: high impact on enantiomeric stability
Albalat, Muriel,Belot, Vincent,Bossa, Giulia,Farran, Daniel,Jean, Marion,Roussel, Christian,Vanthuyne, Nicolas
, p. 16039 - 16047 (2021/09/22)
Based on aN-arylthiazoline scaffold, 22 structures with a N-Carylchiral axis were synthesized exhibiting a huge molecular diversity for the four flanking substituents around the pivotal bond. The determination of their corresponding rotational
Intra- and Intermodular C-S bond formation using a single catalytic system: First direct access to arylthiobenzothiazoles
Murru, Siva,Ghosh, Harisadhan,Sahoo, Santosh K.,Patel, Bhisma K.
supporting information; experimental part, p. 4254 - 4257 (2010/01/06)
We have for the first time developed two llgand-assisted Cu(I)-catalyzed sequential Intra- and intermolecular 5-arylations leading to the direct synthesis of arylthiobenzothlazoles In one pot without an Inert atmosphere. Low catalyst loading, inexpensive
A one-pot preparation of cyanamide from dithiocarbamate using molecular iodine
Nath, Jayashree,Patel, Bhisma K.,Jamir, Latonglila,Sinha, Upasana Bora,Satyanarayana
supporting information; experimental part, p. 1503 - 1506 (2010/05/18)
An efficient one-pot method for the synthesis of cyanamides from dithiocarbamate salts via a double desulfurization strategy using molecular iodine is disclosed. Dithiocarbamates, by the action of iodine yield isothiocyanates in situ, which on treatment with aqueous NH3 give thioureas. The thioureas so generated undergo further oxidative desulfurization with I2 giving corresponding cyanamides in good yields. Environmental benignity, cost effectiveness and high yields are the important attributes of this one pot procedure. The Royal Society of Chemistry 2009.
Axially chiral N-(o-aryl)-2-thioxo-oxazolidine-4-one and rhodanine derivatives: enantiomeric separation and determination of racemization barriers
Yilmaz, Esra Muejde,Dogan, Ilknur
experimental part, p. 2184 - 2191 (2009/04/11)
Axially chiral 5,5-dimethyl-3-(o-aryl)rhodanine, 3-(o-aryl)rhodanine and 5,5-dimethyl-3-(o-aryl)-2-thioxo-4-oxazolidinone derivatives have been synthesized as racemates and the energy barriers to enantiomerization have been determined by dynamic 1/s
