- Discovery of quinazolinyl-containing benzamides derivatives as novel HDAC1 inhibitors with in vitro and in vivo antitumor activities
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A series of quinazolinyl-containing benzamide derivatives were designed, synthesized and evaluated for their in vitro histone deacetylase 1 (HDAC1) inhibitory activities. Compounds 11a surpassed the known class I selective HDAC inhibitor MS-275 in both HDAC1 enzymatic inhibitory activity and cellular anti-proliferative activity against a selected set of cancer cell types (Hut78, K562, Hep3B and HCT116 cells) with no observed effects on human normal cells. In particular, compound 11a inhibited HDAC1 over the other tested HDACs isoforms (HDAC2, HDAC6 and HDAC8) with acceptable safety profiles. Moreover, compound 11a displayed favorable oral pharmacokinetic properties and showed significant antitumor activity in the A549 tumor xenograft model in vivo.
- Zhang, Zixue,Zhang, Qingwei,Zhang, Hao,Jiao, Minru,Guo, Zheng,Peng, Xinyan,Fu, Lei,Li, Jianqi
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- 4-Amino quinazoline compound as well as preparation method and application thereof
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The invention relates to a 4-amino quinazoline compound as well as a preparation method and application thereof. The compound has a general formula I) as shown in the specification, a quinazoline compound is taken as a basis, an aromatic ring methylene is introduced into the system for synthesizing a series of aromatic ring-containing methylene substituted 4-amino quinazoline compounds, the compound has a good inhibiting effect on pathogenic bacteria of plants, and has a good inhibiting effect on pathogenic bacteria such as xanthomonas oryzae, Xanthomonas citri and the like.
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Paragraph 0061; 0062
(2019/05/16)
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- 4-aminoquinazoline grafted acrylamide compounds, preparation method and application thereof
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The invention relates to 4-aminoquinazoline grafted acrylamide compounds, a preparation method and application thereof. The compounds have a structure shown as general formula (I) in the specification. According to the invention, a quinazoline compound is adopted as the basis, and acrylamido is introduced into the system to synthesize a series of acrylamido-containing substituted 4-aminoquinazoline compounds, and the compounds have a good inhibiting effect on plant pathogenic bacteria, and have good inhibiting effect on pathogenic bacteria directed at Xanthomonas oryzae pv. Oryzae, Xanthomonasaxonopodis pv. Citri, etc.
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Paragraph 0070; 0071
(2020/01/12)
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- A 4-N-substituted-5-chloriquine Trifluoromethylbiphenglyl compound and its preparation method and application
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The invention discloses a preparation method and biological activity of a compound with a function of resisting plant germs, 4-N-substituted-5-chloroquinazoline compound which is a compound represented by the general formulas (I) and (II) and a preparation method thereof. According to the invention, the 4-N-substituted-5-chloroquinazoline derivative is synthesized via three or five steps by adopting 2-amino-6-chlorobenzoic acid, formamide, phosphoryl chloride, concentrated hydrochloric acid, N-Boc piperazine and substituted benzyl chloride or benzyl bromine as raw materials and adopting sodium hydride, triethylamine and potassium carbonate as catalysts. The compounds I2, I4, I8 and II5 disclosed by the invention have relatively good inhibiting effects on plant fungi, and the compounds II1, II7, II10, II11, II16 and II17 show relatively high bacteriostatic activity on plant bacteria.
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Paragraph 0089; 0092; 0093
(2017/01/19)
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