7725-93-1Relevant academic research and scientific papers
Synthesis, X-ray analysis, biological evaluation and molecular docking study of new thiazoline derivatives
Mabkhot, Yahia N.,Algarni,Alsayari, Abdulrhman,Muhsinah, Abdullatif Bin,Kheder, Nabila A.,Almarhoon, Zainab M.,Al-Aizari, Faiz A.
, (2019/05/24)
A series of new thiazoline derivatives were synthesized. Structure analyses were accomplished employing1H-NMR,13C-NMR, X-ray and MS techniques. The in vitro antitumor activities were assessed against human hepatocellular carcinoma (HepG-2) and colorectal carcinoma (HCT-116) cell lines. The results revealed that the thiazolines 5b and 2c exhibited significant activity against the two cell lines. The in vitro antimicrobial screening showed that the thiazolines 2c, 5b and 5d showed promising inhibition activity against Salmonella sp. Additionally, the inhibition activity of thiazolines 2e and 5b against Escherichia coli was comparable to that of the reference compound gentamycin.
Dual Inhibition of Mnk2 and FLT3 for potential treatment of acute myeloid leukaemia
Diab, Sarah,Abdelaziz, Ahmad M.,Li, Peng,Teo, Theodosia,Basnet, Sunita K.C.,Noll, Ben,Rahaman, Muhammed H.,Lu, Jingfeng,Hou, Jinqiang,Yu, Mingfeng,Le, Bich T.,Albrecht, Hugo,Milne, Robert W.,Wang, Shudong
, p. 762 - 772 (2017/09/02)
The discovery of novel anti-AML therapeutic agents is urgently needed, but the complex heterogeneity of the disease has so far hampered the development of a curative treatment. FLT3 inhibitors have shown therapeutic potential in clinical trials; but a monotherapy regimen has been associated with resistance mediated by the activation of parallel signalling circuitry, including MAPK and mTOR. Therefore, inhibiting a nexus of the two signalling pathways along with inhibition of FLT3 might be advantageous. Herein, we propose that a dual inhibition of FLT3 and Mnk would provide a better clinical option for AML patients compared to targeting FLT3 alone. Thus, a series of N-phenyl-4-(thiazol-5-yl)pyrimidin-2-amines and 4-(indol-3-yl)-N-phenylpyrimidin-2-amines were prepared. Potent Mnk2 inhibitors, FLT3 inhibitors, and dual inhibitors of Mnk2 and FLT3 were identified and their anti-proliferative activities assessed against MV4-11 AML cell lines. Dual inhibition of FLT3 and Mnk2 caused the increased apoptotic cell death of MV4-11 cells compared to inhibition of FLT3 or Mnk2 alone.
Azole derivatives as histamine H3 receptor antagonists, Part 2: C-C and C-S coupled heterocycles
Walter,Isensee,Kottke,Ligneau,Camelin,Schwartz,Stark
scheme or table, p. 5883 - 5886 (2010/11/18)
With a small series of compounds we demonstrated the variability in the core region of the human histamine H3 receptor (hH3R) antagonist structural blueprint by introducing polar azole groups (oxazole, oxadiazole, thiazole and triazole). Additional variations achieved by coupling different residues to the heterocyclic core structure led to further optimisation of in vitro receptor binding of the novel azole derivatives.
MORPHOLINE COMPOUND
-
Page/Page column 54, (2010/11/27)
A compound represented by the formula (1) wherein ring A is aryl optionally having substituent(s) and the like; ring B is arylene optionally having substituent(s) and the like; m=0-2; n=1-5; X is a bond and the like; Y is a bond and the like; and Z is hydrogen atom and the like or a pharmaceutically acceptable salt thereof, and a hydrate or solvate thereof have affinity for CCR3, and can be pharmaceutical products for the treatment and/or prophylaxis of immune or inflammatory diseases.
A facile synthesis of thiazole-2(3H)-thiones through [hydroxy(tosyloxy) iodo]benzene
Aggarwal, Ranjana,Pundeer, Rashmi,Kumar, Vinod,Chaudhri, Vishwas,Singh, Shiv P.,Prakash, Om
, p. 2659 - 2664 (2007/10/03)
A one-pot facile synthesis of thiazole-2(3H)-thiones (4) has been achieved by hypervalent iodine oxidation of ketones (1) using [hydroxy (tosyloxy)iodo]benzene, followed by the treatment of the reaction mixture with dithiocarbamate salts (3) The intermediate α-tosyloxy-ketones (2) have also been isolated and converted to the target compounds.
Hypervalent iodine in synthesis. 48. A one-pot convenient procedure for the synthesis of 2-mercaptothiazoles by cyclocondensation of ketones with [hydroxy(tosyloxy)iodo]-benzene and ammonium dithiocarbamate
Zhang,Chen
, p. 415 - 420 (2007/10/03)
α-Tosyloxylation of ketones with [hydroxy(tosyloxy)iodo]-benzene (HTIB), followed by treatment with ammonium dithiocarbamate, provides a one-pot convenient procedure for the synthesis of 2-mercaptothiazoles with good yields.
