4036-83-3Relevant articles and documents
Discovery of novel 2-phenylamino-4-prolylpyrimidine derivatives as TRK/ALK dual inhibitors with promising antitumor effects
Cao, Zhi,Guo, Ming,Jiang, Nan,Li, Changtao,Li, Tong,Wang, Xinyu,Yang, Jing,Zhai, Xin
, (2021/10/06)
In order to explore novel TRK and ALK dual inhibitors, a series of 2-phenylamino-4-prolylpyrimidine derivatives were designed, synthesized and evaluated for their in vitro cytotoxicity and enzymatic activities. Delightfully, most compounds were detected m
Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities
Zhu, Huajian,Li, Wenlong,Shuai, Wen,Liu, Yang,Yang, Limei,Tan, Yuchen,Zheng, Tiandong,Yao, Hong,Xu, Jinyi,Zhu, Zheying,Yang, Dong-Hua,Chen, Zhe-Sheng,Xu, Shengtao
, (2021/03/08)
A series of novel N-benzylbenzamide derivatives were designed and synthesized as tubulin polymerization inhibitors. Among fifty-one target compounds, compound 20b exhibited significant antiproliferative activities with IC50 values ranging from 12 to 27 nM against several cancer cell lines, and possessed good plasma stability and satisfactory physicochemical properties. Mechanism studies demonstrated that 20b bound to the colchicine binding site and displayed potent anti-vascular activity. Notably, the corresponding disodium phosphate 20b-P exhibited an excellent safety profile with the LD50 value of 599.7 mg/kg (i.v. injection), meanwhile, it significantly inhibited tumor growth and decreased microvessel density in liver cancer cell H22 allograft mouse model without obvious toxicity. Collectively, 20b and 20b-P are novel promising anti-tubulin agents with more druggable properties and deserve to be further investigated for cancer therapy.
The discovery of novel small molecule allosteric activators of aldehyde dehydrogenase 2
Tian, Wei,Guo, Jiapeng,Zhang, Qingsen,Fang, Shaoyu,Zhou, Ruolan,Hu, Jian,Wang, Mingping,Zhang, Yuefan,Guo, Jin-Min,Chen, Zhuo,Zhu, Ju,Zheng, Canhui
, (2020/12/30)
Aldehyde dehydrogenase 2 (ALDH2) plays important role in ethanol metabolism, and also serves as an important shield from the damage occurring under oxidative stress. A special inactive variant was found carried by 35–45% of East Asians. The variant carriers have recently been found at the higher risk for the diseases related to the damage occurring under oxidative stress, such as cardiovascular and cerebrovascular diseases. As a result, ALDH2 activators may potentially serve as a new class of therapeutics. Herein, N-benzylanilines were found as novel allosteric activators of ALDH2 by computational virtual screening using ligand-based and structure-based screening parallel screening strategy. Then a structural optimization was performed and has led to the discovery of the compound C6. It has good activity in vitro and in vivo, which could reduce infarct size by ～70% in ischemic stroke rat models. This study provided good lead compounds for the further development of ALDH2 activators.
ALDH2 agonist, preparation method and application thereof
-
Paragraph 0135-0137; 0139-0140, (2019/07/10)
The invention belongs to the technical field of medicines, and particularly relates to an ALDH2 agonist, a preparation method and application thereof. The ALDH2 agonist has a novel structure and excellent ALDH2 agonist activity.
N-benzylbenzamide derivatives and preparation method and pharmaceutical application thereof
-
Paragraph 0042-0045, (2019/05/08)
The invention relates to the field of pharmaceutical chemistry, discloses N-benzylbenzamide derivatives with antitumor activity and a preparation method thereof, and further discloses pharmaceutical compositions containing the compounds and application of the compounds or pharmaceutical salts thereof or the compositions containing the compounds to preparation of medicines for treating tumors and inhibiting diseases or symptoms related to tubulin activity.
Discovery of benzoylpiperazines as a novel class of potent and selective GlyT1 inhibitors
Pinard, Emmanuel,Alberati, Daniela,Borroni, Edilio,Fischer, Holger,Hainzl, Dominik,Jolidon, Synese,Moreau, Jean-Luc,Narquizian, Robert,Nettekoven, Matthias,Norcross, Roger D.,Stalder, Henri,Thomas, Andrew W.
scheme or table, p. 5134 - 5139 (2009/05/26)
Screening of the Roche compound library led to the identification of the benzoylpiperazine 7 as a structurally novel GlyT1 inhibitor. The SAR which was developed in this series resulted in the discovery of highly potent compounds displaying excellent sele
Ultrasound-promoted reaction of 2-chlorobenzoic acids and aliphatic amines
Docampo, Maite L.,Pellon, Rolando F.,Estevez-Braun, Ana,Ravelo, Angel G.
, p. 4111 - 4115 (2008/02/13)
An improvement to the use of DMF as a solvent for the condensation of 2-chlorobenzoic acids with aliphatic primary or secondary amines was described. A number of alkylaminobenzoic acids and dialkylaminobenzoic acids were synthesized in acceptable-to-good yield. The advantages of this procedure include readily available substrates, the use of an inexpensive copper powder without taking any precautions to exclude moisture under mild conditions and experimental ease. Furthermore, this condensation could also be achieved under nonclassical conditions by using ultrasonic irradiation at room temperature. We demonstrated that ultrasound-promoted condensation of 2-chlorobenzoic acid with aliphatic amines with the use of DMF as the solvent, especially in the case of secondary amines, affords products in high yields and reduces the reaction time to minutes. The results proved to be highly reproducible because the relevant sonochemical parameters were rigorously controlled. Wiley-VCH Verlag GmbH & Co. KGaA, 2007.
Phenyl-piperazine methanone derivatives, substituted by heterocyclic groups
-
Page/Page column 23, (2008/06/13)
The present invention relates to compounds of the general formula I wherein R1 is the group and R2, R′, R″, R3, R4, R5, R6, R7, X1, X1′, X2, and
Benzoyl-tetrahydropiperidine derivatives
-
Page/Page column 6, (2008/06/13)
The present invention relates to compounds of formula I wherein R1, R2, and Ar; are as defined in the specification. The invention also provides pharmaceutically acceptable acid addition salts thereof and methods for the treatment of
Substituted phenyl methanones
-
Page/Page column 30, (2008/06/13)
The present invention relates to compounds of general formula IA or IB wherein X1 and X2 are each independently N or C—R″ and R1, R2,R3, R4, R5, and R6 are as defined
