- Design, syntheses and antitumor activities evaluation of 1,5-diaryl substituted pyrazole secnidazole ester derivatives
-
According to the drug hybridization principle, a series of novel 1,5-diaryl substituted pyrazole secnidazole ester derivatives (6aa–6gc) have been synthesized by the combinations of various 1,5-diarylpyrazole-3-carboxylic acids with secnidazole. The in vi
- Teng, Qing-Hu,Sun, Gui-Xia,Luo, Shu-Ying,Wang, Kai,Liang, Fu-Pei
-
supporting information
p. 1656 - 1664
(2021/05/29)
-
- When hydrazonoyl chlorides meet terminal alkynes: Regioselective copper(I)-catalysed click sequential reactions to 5-substituted pyrazoles
-
In the presence of catalytic amounts of copper(I) salts, terminal alkynes underwent the formation of copper(I) acetylides that enabled their nucleophilic addition onto hydrazonoyl chlorides followed by spontaneous cyclisation of the resulting alkynylhydrazone intermediate. This sequential reaction sequence was exploited as a facile and regioselective synthesis of 1,3,5-substituted pyrazoles. A catalytic cycle has been proposed accounting for the observed results.
- Molteni, Giorgio
-
p. 1249 - 1259
(2020/09/18)
-
- Design and biological evaluation of novel hybrids of 1, 5-diarylpyrazole and Chrysin for selective COX-2 inhibition
-
The overexpress of COX-2 was clearly associated with carcinogenesis and COX-2 as a possible target has long been exploited for cancer therapy. In this work, we described the design and synthesis of a series of diarylpyrazole derivatives integrating with c
- Ren, Shen-Zhen,Wang, Zhong-Chang,Zhu, Xiao-Hua,Zhu, Dan,Li, Zhang,Shen, Fa-Qian,Duan, Yong-Tao,Cao, Han,Zhao, Jing,Zhu, Hai-Liang
-
p. 4264 - 4275
(2018/07/21)
-
- Bcl-2/MDM2 Dual Inhibitors Based on Universal Pyramid-Like α-Helical Mimetics
-
No α-helical mimetic that exhibits Bcl-2/MDM2 dual inhibition has been rationally designed due to the different helicities of the α-helixes at their binding interfaces. Herein, we extracted a one-turn α-helix-mimicking ortho-triarene unit from o-phenylene foldamers. Linking benzamide substrates with a rotatable C-N bond, we constructed a novel semirigid pyramid-like scaffold that could support its two-turn α-helix mimicry without aromatic stacking interactions and could adopt the different dihedral angles of the key residues of p53 and BH3-only peptides. On the basis of this universal scaffold, a series of substituent groups were installed to capture the key residues of both p53TAD and BimBH3 and balance the differences of the bulks between them. Identified by FP, ITC, and NMR spectroscopy, a compound 6e (zq-1) that directly binds to Mcl-1, Bcl-2, and MDM2 with balanced submicromolar affinities was obtained. Cell-based experiments demonstrated its antitumor ability through Bcl-2/MDM2 dual inhibition simultaneously.
- Wang, Ziqian,Song, Ting,Feng, Yingang,Guo, Zongwei,Fan, Yudan,Xu, Wenjie,Liu, Lu,Wang, Anhui,Zhang, Zhichao
-
supporting information
p. 3152 - 3162
(2016/05/19)
-
- When aryldiazonium salts meet vinyl diazoacetates: A cobalt-catalyzed regiospecific synthesis of N-arylpyrazoles
-
A cobalt-catalyzed C-N bond formation between aryl diazonium salts and vinyl diazoacetates has been developed under relatively mild conditions. The N-arylpyrazoles have been prepared in moderate to high yields in a regiospecific way.
- Guo, Haiheng,Zhang, Daming,Zhu, Chenghao,Li, Jian,Xu, Guangyang,Sun, Jiangtao
-
supporting information
p. 3110 - 3113
(2014/06/23)
-
- New one-pot, efficient, and regioselective method for the synthesis of 3-Trifluoromethyl-1H-1-phenylpyrazoles and alkyl 3-carboxylate analogs
-
An efficient and regioselective procedure for the synthesis of a series of alkyl(aryl/heteroaryl) substituted 3-trifluoromethyl-1H-1-phenylpyrazoles and alkyl 3-carboxylate analogs, from the cyclocondensation reactions of 4-alkoxy-1,1,1-trihaloalk-3-en-2-ones [CX3C(O)CR2=CR 1(OMe/OEt), where R1 = H, Me, Ph, 2-Furyl; R2 = H; R1-R2 = -C4H8- and X = F, Cl] and 1-phenylsemicarbazide in an acidified alcoholic medium (R 3OH/H2SO4), where R3 = Me, Et, Pri was successfully applied and is described here in detail. 2012 Elsevier Ltd. All rights reserved.
- Bonacorso, Helio G.,Correa, Michele S.,Porte, Liliane M.F.,Pittaluga, Everton P.,Zanatta, Nilo,Martins, Marcos A.P.
-
p. 5488 - 5491
(2012/11/07)
-
- Synthesis and herbicidal activity of 1,5-diarylpyrazole derivatives
-
A series of diarylpyrazolecarboxylates and carboxamides were prepared, and their herbicidal activities were investigated. Some of these compounds showed noticeable pre-emergent herbicidal activities against various kinds of weeds. Among the synthesized co
- Kudo, Noriaki,Furuta, Satoru,Taniguchi, Misa,Endo, Takeshi,Sato, Kazuo
-
p. 857 - 868
(2007/10/03)
-
