96103-52-5Relevant academic research and scientific papers
Pyrrole BET degradation agent and application thereof
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, (2022/03/19)
The invention discloses a pyrrole BET degradation agent and application thereof, and belongs to the technical field of biological medicine. The BET protein degradation agent with a brand new parent nucleus structure is provided by adopting a PROTAC technology and comprises a protein target head A, a linker B and an E3 ubiquitination ligase ligand C. The BET protein degradation agent has excellent protein inhibition activity and anti-tumor cell proliferation activity, and compared with an original protein target head compound, the cell activity is greatly improved; and in addition, the preparation method is short in route, and raw materials are cheap and easy to obtain.
Kinetic Target-Guided Synthesis of Small-Molecule G-Quadruplex Stabilizers
Dobia?, Juraj,Dvo?áková, Hana,Hubálek, Martin,Kozák, Jaroslav,Pomeislová, Alice,Reyes-Gutiérrez, Paul E.,Teply, Filip,Veverka, Václav,Vrzal, Luká?
, p. 1236 - 1250 (2020/12/31)
The formation of a G-quadruplex motif in the promoter region of the c-MYC protooncogene prevents its expression. Accordingly, G-quadruplex stabilization by a suitable ligand may be a viable approach for anticancer therapy. In our study, we used the 4-(4-m
NOVEL 5-HYDROXYTRYPTAMINE RECEPTOR 7 ACTIVITY MODULATORS AND THEIR METHOD OF USE
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Paragraph 0263, (2016/06/01)
Pharmaceutical compositions of the invention comprise functionalized lactone derivatives having a disease-modifying action in the treatment of diseases associated with dysregulation of 5-hydroxytryptamine receptor 7 activity.
NOVEL SIGMA-2 RECEPTOR BINDERS AND THEIR METHOD OF USE
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Paragraph 0452, (2016/11/28)
Pharmaceutical compositions of the invention comprise functionalized lactone derivatives having a disease-modifying action in the treatment of diseases associated with dysregulation of sigma-2 receptor activity.
N-aryl-2-aminobenzimidazoles: Novel, efficacious, antimalarial lead compounds
Ramachandran, Sreekanth,Hameed P., Shahul,Srivastava, Abhishek,Shanbhag, Gajanan,Morayya, Sapna,Rautela, Nikhil,Awasthy, Disha,Kavanagh, Stefan,Bharath, Sowmya,Reddy, Jitendar,Panduga, Vijender,Prabhakar,Saralaya, Ramanatha,Nanduri, Robert,Raichurkar, Anandkumar,Menasinakai, Sreenivasaiah,Achar, Vijayashree,Jiménez-Díaz, María Belén,Martínez, María Santos,Angulo-Barturen, I?igo,Ferrer, Santiago,Sanz, Laura María,Gamo, Francisco Javier,Duffy, Sandra,Avery, Vicky M.,Waterson, David,Lee, Marcus C. S.,Coburn-Flynn, Olivia,Fidock, David A.,Iyer, Pravin S.,Narayanan, Shridhar,Hosagrahara, Vinayak,Sambandamurthy, Vasan K.
, p. 6642 - 6652 (2014/10/15)
From the phenotypic screening of the AstraZeneca corporate compound collection, N-aryl-2-aminobenzimidazoles have emerged as novel hits against the asexual blood stage of Plasmodium falciparum (Pf). Medicinal chemistry optimization of the potency against Pf and ADME properties resulted in the identification of 12 as a lead molecule. Compound 12 was efficacious in the P. berghei (Pb) model of malaria. This compound displayed an excellent pharmacokinetic profile with a long half-life (19 h) in rat blood. This profile led to an extended survival of animals for over 30 days following a dose of 50 mg/kg in the Pb malaria model. Compound 12 retains its potency against a panel of Pf isolates with known mechanisms of resistance. The fast killing observed in the in vitro parasite reduction ratio (PRR) assay coupled with the extended survival highlights the promise of this novel chemical class for the treatment of malaria.
RADIOPROTECTOR COMPOUNDS AND METHODS
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Page/Page column 140-141, (2011/10/31)
The invention relates to novel compounds, processes for their preparation and their use in protecting biological materials from radiation damage (radioprotection). Preferred compounds of the invention are those of Formula (II), as follows: wherein W represents -N(R1R2) where R1 and R2 are not both hydrogen and where they may together form a 5, 6 or 7 membered ring structure, -NHN(R1R2), NHR3N(R1R2), -NHR3OR2, -N(R3)R3OR2, -N(R1)R3OR3OR3, OR3NR1R2, -OR3 or W represents piperidyl, piperazinyl, morpholinyl, thiomorpholinyl or diazepanyl each of which may be optionally substituted by C1 to C4 alkyl, C2 to C4 alkenyl, -N(CO)N(R1R2), -N(CO)OR1, -N(CO)OR3OH, -(CO)NR1R2, -R3(CO)NR1R2, -R3OR1, -OR1, -N(R1R2) OR -NH-; R1 and R2 are the or different and are selected from hydrogen, C1 to C4 alkyl or C2 to C4 alkenyl; group or chain; Z is the same or different and represents N or CH; Z' is the same or different and represents N or C; X represents CH, N or NH, where .. is a double bond when X is CH or N and a single bond when X is NH; X' represents N or NH, wherein when X is CH or N X' is NH and wherein X and X' are different and further where ~~~is a double bond when X' is N and a single bond when X' is NH; Q represents H, alkoxyl, -NR1R2, F or Cl; Q1 is absent when Z' is N and when Z' is C it represents H, alkoxyl, -NR1R2, F or Cl; A represents a five to ten membered single or multiple ring structure with heterocyclic N or O located at the ortho position, said ring including optional double bonds, substitutions and/or other heteroatoms and pharmaceutically acceptable derivatives thereof.
Benzimidazole derivatives as new serotonin 5-HT6 receptor antagonists. Molecular mechanisms of receptor inactivation
De La Fuente, Tania,Martín-Fontecha, Mar,Sallander, Jessica,Benhamú, Bellinda,Campillo, Mercedes,Medina, Rocío A.,Pellissier, Lucie P.,Claeysen, Sylvie,Dumuis, Aline,Pardo, Leonardo,López-Rodríguez, María L.
experimental part, p. 1357 - 1369 (2010/08/20)
On the basis of our previously described pharmacophore model for serotonin 5-HT6 receptor (5-HT6R) antagonists, we have designed, synthesized, and pharmacologically characterized a series of benzimidazole derivatives 1-20 that repres
TREATMENT OF MELANOMA
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Page/Page column 40, (2008/12/07)
Methods of treating melanoma include administering a compound of Structure (I), a tautomer of the compound, a pharmaceutically acceptable salt of the compound, a pharmaceutically acceptable salt or the tautomer, or a mixture thereof to a subject. The comp
METHODS FOR TREATING DRUG RESISTANT CANCER
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Page/Page column 66-67, (2008/06/13)
A method for treating drug-resistant cancer, includes: administering to a patient in need thereof, a compound of formula I, a tautomer of the compound, a salt of the compound, a salt of the tautomer, a mixture thereof, or a pharmaceutical composition comp
TREATMENT OF METASTASIZED TUMORS
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Page/Page column 50-51, (2008/06/13)
Methods of treating metastatic cancer such as metastasized tumors include administering a compound of Structure I, a tautomer of the compound, a pharmaceutically acceptable salt of the compound, a pharmaceutically acceptable salt or the tautomer, or a mix
