1793-07-3Relevant articles and documents
A practical solid phase synthesis of quinazoline-2, 4-diones
Shao, Hui,Colucci, Marcus,Tong, Shaojing,Zhang, Hesheng,Castelhano, Arlindo L.
, p. 7235 - 7238 (1998)
We describe a practical solid phase synthesis of quinazoline-2,4-diones using a short-chain, high loading capacity, polyethyleneglycol polystyrene copolymer ('PEG4-PS' resin). The highlights of this synthesis include efficient acyl azide format
Design, synthesis, and biological evaluation of novel quinazolinyl-diaryl urea derivatives as potential anticancer agents
Chen, Jia-Nian,Wang, Xian-Fu,Li, Ting,Wu, De-Wen,Fu, Xiao-Bo,Zhang, Guang-Ji,Shen, Xing-Can,Wang, Heng-Shan
, p. 12 - 25 (2015/11/17)
Through a structure-based molecular hybridization approach, a series of novel quinazolinyl-diaryl urea derivatives were designed, synthesized, and screened for their in vitro antiproliferative activities against three cancer cell lines (HepG2, MGC-803, and A549). Six compounds (7g, 7m, 7o, 8e, 8g, and 8m) showed stronger activity against a certain cell line compared with the positive reference drugs sorafenib and gefitinib. Among the six compounds, 8g exhibited the strongest activity. In particular, compound 8g induced A549 apoptosis, arrested cell cycle at the G0/G1 phase, elevated intracellular reactive oxygen species level, and decreased mitochondrial membrane potential. This compound can also effectively regulate the expression of apoptosis- and cell cycle-related proteins, and influence the Raf/MEK/ERK pathway. Molecular docking and structure-activity relationship analyses revealed that it can bind well to the active site of the receptor c-Raf, which was consistent with the biological data. Therefore, compound 8g may be a potent antitumor agent, representing a promising lead for further optimization.
Discovery of orally bioavailable and novel urea agonists of the high affinity niacin receptor GPR109A
Shen, Hong C.,Szymonifka, Michael J.,Kharbanda, Divya,Deng, Qiaolin,Carballo-Jane, Ester,Wu, Kenneth K.,Wu, Tsuei-Ju,Cheng, Kang,Ren, Ning,Cai, Tian-Quan,Taggart, Andrew K.,Wang, Junying,Tong, Xinchun,Waters, M. Gerard,Hammond, Milton L.,Tata, James R.,Colletti, Steven L.
, p. 6723 - 6728 (2008/04/03)
A urea class of high affinity niacin receptor agonists was discovered. Compound 1a displayed good PK, better in vivo efficacy in reducing FFA in mouse than niacin, and no vasodilation in a mouse model. Compound 1q demonstrated equal affinity to GPR109A as niacin.