220394-97-8Relevant articles and documents
COMPOUND WITH ANTICANCER ACTIVITY
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Paragraph 1409, (2021/01/29)
A compound having anticancer activity, or a pharmaceutically acceptable salt thereof is provided. Used is a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: (wherein, L1 and L2 are the same or different and each represents a group represented by one formula selected from the group consisting of formulas (A) to (F), and S represents a group represented by one formula selected from the group consisting of formulas (S1) to (S18)).
Discovery of 2-substituted 1H-benzo[d]immidazole-4-carboxamide derivatives as novel poly(ADP-ribose)polymerase-1 inhibitors with in?vivo anti-tumor activity
Zhou, Jie,Ji, Ming,Zhu, Zhixiang,Cao, Ran,Chen, Xiaoguang,Xu, Bailing
supporting information, p. 26 - 41 (2017/03/23)
Novel 1H-benzo[d]immidazole-4-carboxamide derivatives bearing five-membered or six-membered N-heterocyclic moieties at the 2-position were designed and synthesized as PARP-1 inhibitors. Structure-activity relationships were conducted and led to a number of potent PARP-1 inhibitors having IC50 values in the single or double digit nanomolar level. Some potent PARP-1 inhibitors also had similar inhibitory activities against PARP-2. Among all the synthesized compounds, compound 10a and 11e displayed strong potentiation effects on temozolomide (TMZ) in MX-1?cells (PF50?=?7.10, PF50?=?4.17). In?vivo tumor growth inhibition was investigated using compound 10a in combination with TMZ, and it was demonstrated that compound 10a could strongly potentiate the cytotoxicity of TMZ in MX-1 xenograft tumor model. Two co-crystal structures of compounds 11b and 15e complexed with PARP-1 were achieved and demonstrated a unique binding mode of these benzo-imidazole derivatives.
2,4-disubstituted [...] compound, and its preparation, and pharmaceutical composition and use thereof
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Paragraph 0703; 0704, (2018/02/04)
The invention discloses new 2,4-disubstituted quinazoline compounds and a preparation method, a medicinal composition and application thereof. The invention particularly relates to 2,4-disubstituted quinazoline compounds shown as a general formula I, medicinal salts thereof, precursors or derivatives thereof with the same biological function, a preparation method thereof, a composition containing one or more of the compounds, and application of the compounds in inhibiting activity of Pin1 enzyme, inhibiting activity of tumor growth and the like.