56341-37-8Relevant articles and documents
Discovery of novel polycyclic spiro-fused carbocyclicoxindole-based anticancer agents
Zhang, Lidan,Ren, Wen,Wang, Xiaoyan,Zhang, Jiaying,Liu, Jie,Zhao, Lifeng,Zhang, Xia
, p. 1071 - 1082 (2016/12/28)
A series of novel polycyclic spiro-fused carbocyclicoxindoles were synthesized and investigated for their in?vitro antiproliferative activities against nine human cancer cell lines. Five compounds (10i, 10l, 10n, 10p, and 10r) demonstrated anticancer activities against A2780s cells with IC50values of less than 30?μM. In particular, compound 10i showed anticancer activities against seven cancer cell lines and stronger activities than cisplatin in A2780s, A2780T, CT26, and HCT116?cells. Further studies illustrated that compound 10i arrested cell cycle in G1 phase and induced apoptosis of HCT116?cells. This compound also effectively increased the protein levels of cleaved caspase-3, p53, and MDM2. Molecular docking results revealed that compound 10i could bind well to the p53-binding site on MDM2, indicating that it might work by blocking the MDM2-p53 interactions.
A Benzisoelenazolone modified pyrrole methyl ester substituted indole ketone compound and use thereof
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Paragraph 0117-0118; 0172-0174, (2016/10/08)
The invention discloses a benzisoselenazolone-modified pyrrolyl formate-substituted indolone compound and a use thereof. The invention depends on and claims the priority of a Chinese patent application 201110105248.0 submitted on April 26, 2011. Through reference, all contents of the Chinese patent application 201110105248.0 are incorporated into the invention. The benzisoselenazolone-modified pyrrolyl formate-substituted indolone compound is shown in the general formula I. The 2-indolone compound provided by the invention has excellent antitumor activity and can be widely used for preparation of antitumor drugs.
Palladium-Catalyzed C-H Activation and Cyclization of Anilides with 2-Iodoacetates and 2-Iodobenzoates: An Efficient Method toward Oxindoles and Phenanthridones
Gandeepan, Parthasarathy,Rajamalli, Pachaiyappan,Cheng, Chien-Hong
, p. 1872 - 1879 (2016/06/15)
A concise approach to the synthesis of oxindoles and phenanthridones from anilides is described. In the presence of catalytic amount of Pd(OAc)2, 2-iodoacetates and 2-iodobenzoates can be used to functionalize ortho C-H bond of anilides, which subsequently undergo intramolecular cyclization to give the products. A possible reaction mechanism that involves a PdII/PdIV catalytic cycle is proposed with the support of detailed mechanistic studies.