943863-69-2Relevant articles and documents
Development of novel bis-pyrazole derivatives as antitumor agents with potent apoptosis induction effects and DNA damage
Dai, Hong,Ge, Shushan,Guo, Jing,Chen, Shi,Huang, Meiling,Yang, Jiaying,Sun, Siyu,Ling, Yong,Shi, Yujun
, p. 1066 - 1076 (2017/12/15)
A series of bis-pyrazole derivatives were designed and synthesized, and their antitumor effects in vitro and in vivo were investigated. Several compounds displayed good antiproliferative activity with IC50 values in low-micromolar range against three human cancer cell lines in vitro, superior to 5-FU. The most potent compound 10M selectively inhibited human hepatocellular carcinoma cells but not non-tumor liver cell proliferation in vitro, and significantly triggered SMMC-7721 cell apoptosis by cleavage of both PARP and caspase-3 in a concentration-dependent manner. Further study revealed that the potent activity in the cell growth inhibition and apoptosis induction effects of 10M were related to DNA damage and activation of the p53 signaling pathway. Moreover, 10M showed low acute toxicity to mice and significant growth inhibition of the hepatoma tumor in vivo.
TOSYLACETATE BASED COMPOUNDS AND DERIVATIVES THEREOF AS PHGDH INHIBITORS
-
, (2018/10/19)
The present invention encompasses compounds of formula (I), wherein the groups R1 to R, A1 to A4 and n have the meanings given in the claims and specification, their use as inhibitors of PHGDH, pharmaceutical compositions
1. 3, 5 - tri-substituted pyrazole compound and its preparation method and application
-
Paragraph 0122; 0123; 0124; 0125, (2017/04/18)
The invention discloses 1,3,5-trisubstituted pyrazole compounds, and a preparation method and application thereof. The structure of the compounds is shown as a general formula (I), and in the general formula (I), R1 is hydrogen, halogens, methyl or triflu
Synthesis and biological evaluation of 3-(4-fluorophenyl)-1H-pyrazole derivatives as androgen receptor antagonists
Guo, Guangzhu,Liu, Jianzhen,Wang, Guanjie,Zhang, Daoguang,Lu, Jinjie,Zhao, Guisen
, p. 278 - 285 (2016/03/30)
A novel series of 3-(4-fluorophenyl)-1H-pyrazole derivatives were synthesized and evaluated for their antiproliferative activity against two prostate cancer cell lines (LNCaP and PC-3) and androgen receptor target gene prostate-specific antigen (PSA) inhibitory activity in LNCaP cells. Several compounds showed potent antiproliferative activity against LNCaP cells and showed a promising PSA downregulation rate. Among these, compound 10e selectively inhibited LNCaP cell growth with an IC50 value of 18 μmol/l and showed a PSA downregulation rate of 46%, which was better than the lead compound T3.
PYRAZOLOALKYL SUBSTITUTED IMIDAZO RING COMPOUNDS AND METHODS
-
Page/Page column 91, (2008/06/13)
Imidazo ring compounds, (e.g., imidazo[4,5-c]quinoline, 6,7,8,9-tetrahydro imidazo[4,5-c]quinoline, imidazo[4,5-c]naphthyridine, 6,7,8,9-tetrahydro imidazo[4,5-c]naphthyridine and imidazo[4,5-c]pyridine compounds) having a pyrazoloalkyl substituent at the