1217655-90-7Relevant articles and documents
Discovery of 2-(1-(3-(4-Chloroxyphenyl)-3-oxo-propyl)pyrrolidine-3-yl)-1H-benzo[d]imidazole-4-carboxamide: A Potent Poly(ADP-ribose) Polymerase (PARP) Inhibitor for Treatment of Cancer
Min, Rui,Wu, Weibin,Wang, Mingzhong,Tang, Lin,Chen, Dawei,Zhao, Huan,Zhang, Cunlong,Jiang, Yuyang
, (2019)
A series of benzimidazole carboxamide derivatives have been synthesized and characterized by 1H-NMR, 13C-NMR and HRMS. PARP inhibition assays and cellular proliferation assays have also been carried out. Compounds 5cj and 5cp exhibited potential anticancer activities with IC50 values of about 4 nM against both PARP-1 and PARP-2, similar to the reference drug veliparib. The two compounds also displayed slightly better in vitro cytotoxicities against MDA-MB-436 and CAPAN-1 cell lines than veliparib and olaparib, with values of 17.4 μM and 11.4 μM, 19.8 μM and 15.5 μM, respectively. The structure-activity relationship based on molecular docking was discussed as well.
HETEROCYCLIC SPIRO-COMPOUNDS AS AM2 RECEPTOR INHIBITORS
-
Page/Page column 148; 305, (2020/06/05)
Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: wherein R1, R2, R4, R5, R6, R7, R8, R9, R10,Z, X1, X2, X3, L2, HET, n and q are as defined herein. The compounds are inhibitors of adrenomedullin receptor subtype 2 (AM2). Also disclosed are the compounds for use in the treatment of diseases modulated AM2, including proliferative diseases such as cancer; pharmaceutical compositions comprising the compounds; methods for preparing the compounds; and intermediates useful in the preparation of the compounds.
With antifungal activity of the wicked zuozuo apperception compound and its preparation method and application (by machine translation)
-
Paragraph 0040-0042, (2017/09/02)
The invention discloses an oxazole compound with anti-fungal activity, a preparation method of the oxazole compound and an application of the oxazole compound to tobacco powdery mildew original fungi or cotton anthracnose original fungi prevention, and belongs to the technical field of organic synthesis. The technical scheme mainly includes that the oxazole compound with the anti-fungal activity is provided with a structure shown in the instruction, R1 refers to propiono, isopropyl, acetyl, ethyl or methyl, and R2 refers to dimethylamino or methylamine. Five oxazole compounds with the anti-fungal activity are synthesized by the novel method, the preparation process is simple in technology and easy to control, target product yield is high, repeatability is fine, and the five prepared oxazole compounds with the anti-fungal activity have a certain prevention function for tobacco powdery mildew original fungi or cotton anthracnose original fungi.