6219-49-4Relevant academic research and scientific papers
Synthesis and evaluation of bioactivity of thiazolo[3,2-b]-[1,2,4]- triazoles and isomeric thiazolo[2,3-c]-[1,2,4]-triazoles
Kumar,Kumar,Makrandi
, p. 1223 - 1229 (2013)
Synthesis of 2-(o-nitrophenyl)-6-arylthiazolo[3,2-b]-[1,2,4]-triazoles 4 and its isomer 3-(o-nitrophenyl)-5-arylthiazolo[2,3-c]-[1,2,4]-triazoles 6 has been achieved starting from the appropriate 1-(o-nitrobenzoyl)-3- thiosemicarbazide 1. Compound 1 on co
Dammarane sapogenin derivative and preparation method and application thereof
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, (2020/10/04)
The invention belongs to the technical field of medicines, and relates to a dammarane sapogenin derivative and a preparation method and application thereof. A series of dammarane sapogenin derivativesare obtained by combining dammarane sapogenins from plants with different groups. Anticancer activity evaluation and anticancer activity mechanism research are carried out on the derivative, and results show that the prepared dammarane sapogenin derivative has a remarkable anticancer effect, has no toxic effect on normal cells and can be used for preparing drugs for treating cancers.
Novel panaxadiol triazole derivatives induce apoptosis in HepG-2 cells through the mitochondrial pathway
Xiao, Shengnan,Wang, Xude,Xu, Lei,Li, Tao,Cao, Jiaqing,Zhao, Yuqing
, (2020/07/23)
In this study, we introduced 1, 2, 4-triazole groups into panaxadiol (PD) to obtain 18 panaxadiol triazole derivatives. Five cancer cells and one normal cell were evaluated for cytotoxicity by MTT assay. The results showed that most of the derivatives could inhibit cancer cell proliferation, and the anti-proliferative activity of compound A1 was the most significant. For HepG-2 cells, the IC50 value was 4.21 ± 0.54 μM, which was nearly 15 times higher than the activity of PD. Further studies showed that compound A1 could induce apoptosis in HepG-2 cells, and could enhance the expression of Cl-caspase-3, Cl-caspase-9 and Cl-PARP. Moreover, Western blot analysis showed that after treating HepG-2 cells with compound A1, the expression of p53 protein was increased and the ratio of Bax/Bcl-2 was gradually increased. The cytoplasmic Bax is then translocated to the mitochondria, causing the release of Cyt c protein. Therefore, the results indicate that compound A1 induces apoptosis through the mitochondrial pathway and can be used the potential to develop new anti-proliferative agents.
Synthesis, hypoglycemic and hypolipidemic activities of novel thiazolidinedione derivatives containing thiazole/triazole/oxadiazole ring
Mohammed Iqbal,Khan, Ashraf Y.,Kalashetti, Mallikarjun B.,Belavagi, Ningaraddi S.,Gong, Young-Dae,Khazi, Imitiyaz Ahmed M.
body text, p. 308 - 315 (2012/08/08)
Novel thiazolidinedione derivatives were synthesized by incorporating pharmacologically significant heterocycles viz, substituted thiazole, triazole, and oxadiazole moieties linked to the central phenyl ring via heteroatomlinkage with one/two carbon spacer as the structural analogs of Pioglitazone by employing multistep synthetic protocols. Structures of all the newly synthesized intermediates and target molecules were established by analytical and spectral data. These newly synthesized compounds were screened for their invivo hypoglycemic and hypolipidemic activities in male wistar rats. Some of the synthesized compounds demonstrated good activity.
Trimethylsilyl isothiocyanate (TMSNCS): An efficient reagent for the one-pot synthesis of mercapto-1,2,4-triazoles
Guda, Dinneswara Reddy,Wang, Tengjiao,Cho, Hyeon Mo,Lee, Myong Euy
supporting information, p. 5238 - 5242 (2012/11/07)
A mild, convenient, and efficient one-pot synthesis of mercapto-1,2,4- triazoles is described. Various hydrazides efficiently reacted with trimethylsilyl isothiocyanate (TMSNCS) under basic condition to give mercapto-1,2,4-triazoles in high yields.
