32618-85-2Relevant academic research and scientific papers
Synthesis, spectroscopic characterization and x-ray analysis of 6-nitroquinazoline-2,4(1H,3H)-dione
Kesternich, Victor,Perez-Fehrmann, Marcia,Ortiz, Sergio,Verdugo, Felipe,Brito, Ivan,Bolte, Michael,Cardenas, Alejandro
, p. 1817 - 1819 (2013)
In this work, 6-nitroquinazoline-2,4(1H,3H)-dione was obtained in two step with good yields using a facile synthetic method. Its structure was characterized by X-ray single crystal diffraction technique (XRD), IR, 1D-NMR (1H-NMR and 13C-NMR) and 2D-NMR (H-H COSY and H-C HMBC) spectroscopy. All N and O carbonyl atoms are involved in hydrogen bonding, with an average HO distance of 1.89(2) A and N-HO angles in the range 169.5(2)-177.2(2). In the crystal packing the molecules are associated by two strong intermolecular N-HO hydrogen bonds forming centrosymmetric ring with graph-set motif R22(8), which are linked by N-HO hydrogen bonds.
Transition metals in organic synthesis, part 111: 1 first total synthesis and structural revision of antipathine A
Berndt, Andreas,Gruner, Margit,Schmidt, Arndt W.,Kn?lker, Hans-Joachim
, p. 2102 - 2106 (2013)
We describe the first total synthesis of antipathine A and a revision of the original structural assignment. Georg Thieme Verlag Stuttgart, New York.
DIACYLGLYCEROL KINASE MODULATING COMPOUNDS
-
Page/Page column 1301, (2021/07/02)
The present disclosure provides diacylglycerol kinase modulating compounds, and pharmaceutical compositions thereof, for treating cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection. The compounds can be used alone or in combination with other agents.
Synthesis and Anti-Proliferation Activity Evaluation of Novel 2-Chloroquinazoline as Potential EGFR-TK Inhibitors
Zheng, Quan,Xu, Xuan-Bo,Jin, Hao,Zhang, Wen,Rao, Guo-Wu
, (2021/10/23)
A novel series of 2-chloroquinazoline derivatives had been synthesized and their anti-proliferation activities against the four EGFR high-expressing cells A549, NCI-H1975, AGS and HepG2 cell lines were evaluated. The preliminary SAR study of the scaffold of new compounds showed that the compounds with a chlorine substituent on R3 had a better anti-proliferation activity than those substituted by hydrogen atom or vinyl group. Among them, 2-chloro-N-[2-chloro-4-(3-chloro-4-fluoroanilino)quinazolin-6-yl]acetamide (10b) had the best activity, and the corresponding IC50 were 3.68, 10.06, 1.73 and 2.04 μM, respectively. And compound 10b had better or equivalent activity against four cell lines than Gefitinib. The activity of the compound 10b on the EGFR enzyme was subsequently tested. The Wound Healing of A549, AGS and HepG2 cells by this compound showed that the compound can inhibit the migration of cancer cells. Finally, the action channel of the compound 10b was supported by western blotting experiments. It provides useful information for the design of EGFR-TK inhibitors.
3-benzyl-6-amido-2, 4-(1H, 3H)-quinazolinedione derivatives and synthesis method and application thereof
-
Paragraph 0014; 0018; 0020; 0021, (2019/06/12)
The present invention relates to 3-Benzyl-6-Amido-2, 4-(1H,3H)-quinazolinedione derivatives and synthesis methods and application thereof, belongs to the technical field of medicine, and relates to ageneral formula (I), wherein R1, R2 and R3 are different
4-AMINO-2-PYRIDO-BICYCLIC PYRIMIDINES AND USE THEREOF AS TOPOISOMERASE II INHIBITORS
-
Page/Page column 22; 52-53, (2018/07/29)
The present invention concerns 4-amino-2-pyrido-bicyclic pyrimidines as type II topoisomerase inhibitors and use thereof as medicaments especially in the treatment of cancer. The invention also provides a method for the manufacture of 4- amino-2-pyrido bicyclic pyrimidines.
Identification of novel quinazolinedione derivatives as RORγt inverse agonist
Fukase, Yoshiyuki,Sato, Ayumu,Tomata, Yoshihide,Ochida, Atsuko,Kono, Mitsunori,Yonemori, Kazuko,Koga, Keiko,Okui, Toshitake,Yamasaki, Masashi,Fujitani, Yasushi,Nakagawa, Hideyuki,Koyama, Ryoukichi,Nakayama, Masaharu,Skene, Robert,Sang, Bi-Ching,Hoffman, Isaac,Shirai, Junya,Yamamoto, Satoshi
, p. 721 - 736 (2018/02/07)
Novel small molecules were synthesized and evaluated as retinoic acid receptor-related orphan receptor-gamma t (RORγt) inverse agonists for the treatment of inflammatory and autoimmune diseases. A hit compound, 1, was discovered by high-throughput screeni
CO2 transformation under mild conditions using tripolyphosphate-grafted KCC-1-NH2
Sadeghzadeh, Seyed Mohsen,Zhiani, Rahele,Moradi, Marjan
, p. 535 - 544 (2018/04/26)
Fibrous nanosilica (KCC-1) as a catalyst support was investigated in terms of stability, recycling, and reusability. For the first time, CO2 transformation was performed via the synthesis and application of KCC-1 together with sodium tripolyphosphate (STPP) and 3-aminopropyltriethoxysilane (APTES) as its functionalized derivative. To this goal, KCC-1/STPP NPs were applied to act as a nanocatalyst with excellent catalytic activities under green reaction conditions.
HETEROCYCLIC COMPOUND
-
Paragraph 0461, (2017/08/01)
The problem of the present invention is to provide a compound having a superior RORγt inhibitory action, and useful as a prophylactic or therapeutic agent for psoriasis, inflammatory bowel disease, ulcerative colitis, Crohn's disease, rheumatoid arthritis, multiple sclerosis, uveitis, asthma, ankylopoietic spondylarthritis, systemic lupus erythematosus, chronic obstructive pulmonary disease or the like. The present invention relates to a compound represented by the formula (I): [wherein each symbol is as described in the DESCRIPTION] or a salt thereof, which has an RORγt inhibitory action, and useful as a prophylactic or therapeutic agent for psoriasis, inflammatory bowel disease, ulcerative colitis, Crohn's disease, rheumatoid arthritis, multiple sclerosis, uveitis, asthma, ankylopoietic spondylarthritis, systemic lupus erythematosus, chronic obstructive pulmonary disease or the like.
Coumarins and other fused bicyclic heterocycles with selective tumor-associated carbonic anhydrase isoforms inhibitory activity
Bozdag, Murat,Alafeefy, Ahmed Mahmoud,Altamimi, Abdul Malik,Vullo, Daniela,Carta, Fabrizio,Supuran, Claudiu T.
, p. 677 - 683 (2016/12/27)
Herein we report for the first time a series of 2-benzamido-N-(2-oxo-4-(methyl/trifluoromethyl)-2H-chromen-7-yl) benzamide 3a–f and substituted quinazolin-4(3H)-ones and 2H-benzo[e][1,2,4]thiadiazin-3(4H)-one 1,1-dioxides (5, 6, 8 and 10a–c) as selective inhibitors of the tumor associated hCA IX and XII isoforms. Among the compounds reported the trifluoromethyl derivative 3d resulted the most potent against these CA isoforms with KIs of 10.9 and 6.7?nM.
