91687-70-6Relevant academic research and scientific papers
Synthesis and Investigation of S-Substituted 2-Mercaptobenzoimidazoles as Inhibitors of Hedgehog Signaling
Gr??le, Simone,Susanto, Steven,Sievers, Sonja,Tavsan, Emel,Nieger, Martin,Jung, Nicole,Br?se, Stefan
supporting information, p. 931 - 935 (2017/09/22)
Due to the arising resistance of common drugs targeting the Hedgehog signaling pathway, the identification of new compound classes with inhibitory effect is urgently needed. We were able to identify S-alkylated 2-mercaptobenzoimidazoles as a new compound
Synthesis of salicylic acid-based 1,3,4-oxadiazole derivatives coupled with chiral oxazolidinones: Novel hybrid heterocycles as antitumor agents
Murty,Penthala, Raju,Nath, Lekshmi R.,Anto, Ruby John
, p. 1133 - 1142 (2015/03/31)
A series of novel salicylic acid-based 1,3,4-oxadiazoles derivatives coupled with chiral oxazolidinones were synthesized to screen for their in vitro antitumor activity against five human cancer cell lines. Some of these compounds showed good antitumor activities with IC50values ranging from 31.19-57.21 μM. Among the tested compounds 11, 15, 19,23,24, and 34 showed broad-spectrum antitumor activity against all the cell lines. In particular, compound 19 revealed remarkable antitumor activity with IC50 = 31.19-41.87 μM. A431 was the most sensitive cell line against all the compounds studied, followed by HeLa, MCF-7, A549 and HepG2. Structures of newly synthesized compounds were confirmed by IR,1 H NMR, 13C NMR and HRMS spectral data
Synthesis and relaxivity measurement of cyclen based magnetic resonance imaging (MRI) contrast agent
Ur Rashid, Haroon,Khan, Khalid,Yaseen, Muhammad,Hassan, Waseem,Naveed Umar, Muhammad
, p. 27 - 33 (2015/12/23)
1, 4, 7, 10-teraazacyclododecane (cyclen) is a key macrocycle used for the synthesis of Magnetic Resonance Imaging (MRI) contrast agents. Substituting the hydrogen atoms (attached to the nitrogen atoms in the ring) of cyclen with suitable groups produce stable ligands. These ligands on complexation with Ln3+ ions lead to the formation of useful chelates. Cyclen is widely synthesized via Richman and Atkins method. Cyclen based ligand 1,4,7-tris(carboxymethyl)-10-(methyl,2-ethoxybenzoate)- 1,4,7,10-tetraazacyclododecane (DO3A-MEB) was synthesized in this work. It was subsequently coupled with Gd3+ ion to afford its stable complex. Relaxivity of the complex was measured by inversion recovery (IR) method and it was compared with that of the commonly used MRI contrast agent Gd-DTPA. Longitudinal relaxivity measurements indicated 128 % enhancement compared to Gd-DTPA.
9-SUBSTITUTED 8-OXOADENINE COMPOUND
-
Page/Page column 119, (2010/11/24)
The present invention provides an 8-oxoadenine compound having immunemodulating activities such as an interferon inducing activity and useful as an antiviral agent and antiallergic agent, which is represented by the following formula (1): [wherein the ring A represents a 6-10 membered aromatic carbocyclic ring and the like, R represents a halogen atom, an alkyl group and the like, n represents an integer of 0-2, Z 1 represents alkylene, X 2 represents oxygen atom, sulfur atom, SO 2 , NR 5 , CO, CONR 5 , NR 5 CO and the like, Y 1 , Y 2 and Y 3 represent independently a single bond or an alkylene group, X 1 represents oxygen atom, sulfur atom, NR 4 (R 4 is hydrogen atom or an alkyl group) or a single bond, R 2 represents a substituted or unsubstituted alkyl group, R 1 represents hydrogen atom, hydroxy group, an alkoxy group, an alkoxycarbonyl group or a haloalkyl group] or its pharmaceutically acceptable salt.
Pyrimidin derivatives
-
, (2008/06/13)
The invention relates to new pharmaceutically active compounds which are are P2-purinoceptor 7-transmembrane (TM) G-protein coupled receptor antagonists, compositions containing them and processes for their preparation.
AMP deaminase inhibitors. 3. SAR of 3-(carboxyarylalkyl)coformycin aglycon analogues
Kasibhatla, Srinivas Rao,Bookser, Brett C.,Probst, Gary,Appleman, James R.,Erion, Mark D.
, p. 1508 - 1518 (2007/10/03)
N3-Substituted coformycin aglycon analogues with improved AMP deaminase (AMPDA) inhibitory potency are described. Replacement of the 5-carboxypentyl substituent in the lead AMPDA inhibitor 3-(5-carboxypentyl)-3,6,7,8- tetrahydroimidazo[4,5-d][1,3]diazepin-8-ol (2) described in the previous article with various carboxyarylalkyl groups resulted in compounds with 10- 100-fold improved AMPDA inhibitory potencies. The optimal N3 substituent had m-carboxyphenyl with a two-carbon alkyl tether. For example, 3-[2-(3-carboxy- 5-ethylphenyl)ethyl]-3,6,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-8-ol (43g) inhibited human AMPDA with a K(i) = 0.06 μM. The compounds within the series also exhibited > 1000-fold specificity for AMPDA relative to adenosine deaminase.
