4542-46-5Relevant articles and documents
Novel pyrimido-heterocyclic compound and preparation method and application thereof
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Paragraph 0194; 0196; 0197; 0198; 0199, (2019/02/19)
The invention discloses a novel pyrimido-heterocyclic compound and a preparation method and application thereof. The structure of the pyrimido-heterocyclic compound disclosed by the invention is as shown in a general formula I, and the definitions of all substituents are described in the specification and claims. The pyrimido-heterocyclic compound disclosed by the invention has much better inhibitory activity and selectivity for double-mutant EGFR kinase than the existing AZD-9291, can be used for preparing anti-tumor drugs, and overcomes the defect of drug tolerance of the first generation ofEGFR inhibitor.
Design, synthesis and biological evaluation of novel podophyllotoxin derivatives bearing 4β-disulfide/trisulfide bond as cytotoxic agents
Zhu, Shi-Jun,Ying, Hua-Zhou,Wu, Yan,Qiu, Ni,Liu, Tao,Yang, Bo,Dong, Xiao-Wu,Hu, Yong-Zhou
, p. 103172 - 103183 (2015/12/23)
A novel series of C-4β-disulfide/trisulfide-containing podophyllotoxin derivatives were designed, synthesized, and biologically evaluated for their cytotoxic activities against human cancer cell lines, including KB (Mouth Epidermal Carcinoma Cells) and KB/VCR (Vincristine-resistant Mouth Epidermal Carcinoma Cells). Most of these compounds exhibited promising moderate to good cytotoxic activities. In particular, some of them displayed even superior activities to that of etoposide, especially for KB/VCR cell lines, indicating that introduction of the disulfide/trisulfide moiety would be beneficial for overcoming the multi-drug resistant limitation of etoposide. Moreover, the metabolic evaluation of the most promising compound was further performed to reveal that disulfide bond can be stable in human plasma over 8 hours, indicating good potential of these compounds for in vivo anti-cancer activities.
NOVEL CYCLOSPORIN DERIVATIVES AND USES THEREOF
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Paragraph 0369-0370, (2014/09/29)
The present invention relates to a compound of the Formula (I)): or pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same, a method for treating or preventing viral infections, inflammation, dry eye, central nervous disorders, cardiovascular diseases, cancer, obesity, diabetes, muscular dystrophy, and hair loss.