96103-52-5Relevant articles and documents
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.
NOVEL 5-HYDROXYTRYPTAMINE RECEPTOR 7 ACTIVITY MODULATORS AND THEIR METHOD OF USE
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, (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.
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.