107275-54-7Relevant articles and documents
Synthesis of novel aryl dithian valeryl podophyllotoxin ester derivatives as potential antitubulin agents
Lin, Hong-Yan,Li, Zi-Kang,Han, Hong-Wei,Qiu, Han-Yue,Gu, Hong-Wei,Yang, Yong-Hua,Wang, Xiao-Ming
, p. 47511 - 47521 (2015)
Microtubules are among the most successful targets for anticancer therapy. In this study, we described the synthesis routes of the lipoyl podophyllotoxin ester derivatives and found that they can selectively inhibit the proliferation of cancer cells without damaging the non-cancer cells. Among them, L4 showed the best antiproliferation activity with IC50 = 2.68 μM against A549 cells. This effect of L4 was similar to that of CA-4 (IC50 = 2.78 μM), a typical microtubule inhibitor, but better than podophyllotoxin (IC50 = 6.57 μM) itself. Furthermore, cell cycle analysis revealed that L4 can remarkably cause cell cycle arrest in the G2/M phase in a time- and dose-dependent manner. But the effect of L4 on apoptosis inducing was not apparent enough. Moreover, confocal microscopy and western blot analysis results indicated that L4 can perturb microtubule polymerization, thus causing tumor growth inhibition.
Thioctic acid aldehyde derivatives, and preparation method and application thereof
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Paragraph 0051-0054, (2019/11/20)
The invention belongs to the technical field of chemical pharmacy, and concretely relates to thioctic acid aldehyde derivatives, a preparation method thereof, and an application of the thioctic acid aldehyde derivatives in the preparation of antitumor drugs as a histone deacetylase inhibitor. Aldehyde compounds are introduced into thioctic acid molecules by chemical synthesis to obtain the thioctic acid aldehyde compounds with a novel structure, and a result of in-vitro antitumor activity study shows that the thioctic acid aldehyde derivative has a significant inhibition effect on the tumor cells OVCaR-3, A549 and NCI-H460. From the perspective of the activity results and the preparation possibility, the thioctic acid aldehyde derivatives can be processed to prepare high-efficiency and low-toxicity antitumor drugs, and have broad drug development prospects.
Synthesis of Dithioacetals from Carbonyl Compounds and Thiols in the Presence of Polyphosphoric Acid Trimethylsilyl Ester (PPSE)
Kakimoto, Masa-aki,Seri, Takuya,Imai, Yoshio
, p. 164 - 166 (2007/10/02)
Dithioacetals were synthesized from carbonyl compounds and thiols in the presence of polyphosphoric acid trimethylsilyl ester (PPSE).Aldehydes, ketones, and trioxane could be used as carbonyl compounds, and aromatic, primary, secondary, and tertiary thiols were applicable in the present reaction.The reaction between cyclohexanone and t-butyl thiol afforded a mixture of corresponding dithioacetal and t-butylcyclohexenylsulfide.