1120331-50-1Relevant academic research and scientific papers
Identification of 4-anilino-6-aminoquinazoline derivatives as potential MERS-CoV inhibitors
Jang, Min Seong,Jin, Young-hee,Kim, Hyoung Rae,Kim, Seungtaek,Kwon, Sunoh,Lee, Jihye,Lee, Jun Young,Park, Chul Min,Shin, Young Sup,Song, Jong Hwan
, (2020/08/19)
New therapies for treating coronaviruses are urgently needed. A series of 4-anilino-6-aminoquinazoline derivatives were synthesized and evaluated to show high anti-MERS-CoV activities. N4-(3-Chloro-4-fluorophenyl)-N6-(3-methoxybenzyl
Discovery of 4,6-substituted-(diaphenylamino)quinazolines as potent c-Src inhibitors
Li, Jing-Ran,Li, Dong-Dong,Fang, Fei,Du, Qian-Ru,Lin, Lin,Sun, Jian,Qian, Yong,Zhu, Hai-Liang
, p. 8375 - 8386 (2013/12/04)
A series of 4,6-substituted-(diaphenylamino)quinazolines as c-Src inhibitors have been prepared and their biological activity has also been evaluated. All the compounds displayed potential antiproliferation activities, with IC50 values ranging from 3.42 μM to 118.81 μM in five human tumor cell lines. Particularly, compound 15 exhibited higher cytotoxicity against the tested five tumor cell lines compared to the other small molecules. Generally, most of these compounds showed selectivity between the A549 cells and the other four cells, according to their corresponding IC50 values. The results obtained from the in vitro enzyme assay indicated compound 15 has remarkable inhibitory activity against c-Src kinase with an IC50 value of 27.3 nM, which is comparable to the control compounds. Furthermore, molecular docking and QSAR study by means of DS 3.5 (Discovery Studio 3.5, Accelrys, Co. Ltd) explored the binding modes and the structure and activity relationship (SAR) of these derivatives.
Design, synthesis and antitumor evaluation of phenyl N-mustard-quinazoline conjugates
Marvania, Bhavin,Lee, Pei-Chih,Chaniyara, Ravi,Dong, Huajin,Suman, Sharda,Kakadiya, Rajesh,Chou, Ting-Chao,Lee, Te-Chang,Shah, Anamik,Su, Tsann-Long
, p. 1987 - 1998 (2011/04/25)
A series of N-mustard-quinazoline conjugates was synthesized and subjected to antitumor studies. The N-mustard pharmacophore was attached at the C-6 of the 4-anilinoquinazolines via a urea linker. To study the structure-activity relationships of these conjugates, various substituents were introduced to the C-4 anilino moiety. The preliminary antitumor studies revealed that these agents exhibited significant antitumor activity in inhibiting various human tumor cell growths in vitro. Compounds 21b, 21g, and 21h were selected for further antitumor activity evaluation against human breast carcinoma MX-1 and prostate PC-3 xenograft in animal model. These agents showed 54-75% tumor suppression with low toxicity (5-7% body-weight changes). We also demonstrate that the newly synthesized compounds are able to induce DNA cross-linking through alkaline agarose gel shift assay and inhibited cell cycle arrest at G2/M phase.
Search for new pharmacophores for antimalarial activity. Part II: Synthesis and antimalarial activity of new 6-ureido-4-anilinoquinazolines
Madapa,Tusi,Mishra,Srivastava,Pandey,Tripathi,Puri,Batra
experimental part, p. 222 - 234 (2011/03/19)
Synthesis of new 6-ureido-4-anilinoquinazolines have been accomplished and their in vitro antimalarial activity against chloroquine-sensitive P. falciparum have been examined. Out of 64 compounds evaluated, the IC50 of 16 compounds which have d
