共查询到20条相似文献,搜索用时 78 毫秒
1.
2.
利用药物设计的拼合原理,以黄体酮为原料,经过氧化开环、闭环、还原及缩合反应等步骤,设计合成了9个目标化合物,其结构经IR、NMR和HR-MS确证。以阿比特龙和5-氟脲嘧啶为阳性对照,采用MTT法初步评价目标化合物对体外人前列腺癌细胞PC-3、人卵巢癌细胞Skov3、人恶性黑色瘤细胞A375和人正常前列腺上皮细胞RWPE-1的抗增殖活性。结果显示,2-氨基-4-吡啶-4-基-6-(4′-氮杂孕甾-3′-酮-17′-基)烟腈、2-氨基-4-呋喃-2-基-6-(4′-氮杂孕甾-3′-酮-17′-基)烟腈对PC-3和Skov3细胞抗增殖活性优于阳性对照药阿比特龙和5-氟脲嘧啶。特别是2-氨基-4-吡啶-4-基-6-(4′-氮杂孕甾-3′-酮-17′-基)烟腈对PC-3细胞的IC50值为(2.73±0.80)μmol/L,明显优于阿比特龙,值得进一步研究。 相似文献
3.
4.
三甲锍硫酸甲酯是一种新型的硫叶立德试剂,将其应用于医药中间体3β羟基-15β,16β亚甲基-17β-螺(环氧乙烷)-雄甾-5-烯的合成中,使用三甲锍硫酸甲酯,其催化剂为固体粉末KOH,而不像其它硫叶立德试剂要用昂贵的NaH作催化剂.成功的合成了目标化合物.产率75.6%,反应条件温和,利于工业化生产,产物经IR,1H-NMR、13C-NMR、MS确定. 相似文献
5.
6.
7.
三甲锍硫酸甲酯是一种新型的硫叶立德试剂,将其应用于医药中间体3β-羟基-15β,16β亚甲基-17β-螺(环氧乙烷)-雄甾-5-烯的合成中,使用三甲锍硫酸甲酯,其催化剂为固体粉末KOH,而不像其它硫叶立德试剂要用昂贵的NaH作催化剂。成功的合成了目标化合物。产率75.6%,反应条件温和,利于工业化生产,产物经IR,^1H—NMR、^13C—NMR、MS确定。 相似文献
8.
以4-氮杂芴-9-酮(IP)为电子受体,咔唑(Cz)为电子供体,通过调节Cz在IP上的取代位置合成了4例荧光染料,即IP-6-Ph Cz、IP-7-PhCz、IP-8-PhCz和IP-9-PhCz。利用紫外吸收光谱、荧光发射光谱、电化学分析等对所得4例荧光染料的光致发光、电致发光以及电化学性质进行了测试。结果表明,IP-6-Ph Cz和IP-9-PhCz分别实现了45.3°和51.8°的大扭曲角,其单重态-三重态能级差(ΔEST)分别为0.32和0.28eV,表现出热活化延迟荧光(TADF)特征,而IP-7-PhCz和IP-8-PhCz仅是普通的荧光染料。其中,IP-7-PhCz的光致发光量子产率(PLQY)为29%,电致发光的最大外量子效率为2.8%。 相似文献
9.
10.
11.
12.
13.
14.
15.
16.
H. Din C. J. Gray J. C. Ireson R. McDonald 《Journal of chemical technology and biotechnology (Oxford, Oxfordshire : 1986)》1991,50(2):181-189
T-Butyloxycarbonyl-α-aza-(4-aminophenyl)alanine phenyl ester (Fig. 1, III: R = NH2) has been synthesized. The rate of inhibition of trypsin (EC 3.4.21.4) by this compound (due to acylation followed by slower deacylation) shows a marked pH maximum at approximately 6. The shape of the pH—rate curve is discussed in terms of (i) the normal pH—activity curve of trypsin reacting with a charged substrate, i.e. the protonated form of the amino compound, (ii) the deprotonation of the 4-amino group with pKa 4·3, and (iii) the lower rate of reaction of the enzyme with the uncharged, deprotonated form of the ester. 相似文献
17.
18.
以3,4-二氟硝基苯为原料,与吗啉在二异丙基乙胺中反应4 h得到3-氟-4-吗啉硝基苯(Ⅰ),在w(Pd)=10%催化下,Ⅰ与甲酸铵在V(THF) V(甲醇)=1 4中反应6 h,得3-氟-4-吗啉苯胺(Ⅱ),Ⅱ与光气在通入干燥HCl气体下反应得3-氟-4-吗啉异氰酸苯酯(Ⅲ),最后在无水LiBr和n-Bu3PO催化下,Ⅲ与(R)-丁酸缩水甘油酯在二甲苯中反应2 h,所得产物在甲醇钠催化下,与甲醇反应3 h,合成了(R)-3-(3-氟-4-吗啉苯基)-2-氧-5-(口恶)唑烷基甲醇(Ⅳ),总收率35.8%. 相似文献
19.
20.
Deore RR Chen GS Chang PT Chern TR Lai SY Chuang MH Lin JH Kung FL Chen CS Chiou CT Chern JW 《ChemMedChem》2012,7(5):850-860
The metal ion chelating β-N-hydroxy-γ-ketocarboxamide pharmacophore was integrated into a quinazolinone scaffold, leading to N-arylalkyl-3-hydroxy-4-oxo-3,4-dihydroquinazolin-2-carboxamide derivatives as hepatitis C virus (HCV) NS5B polymerase inhibitors. Lead optimization led to the identification of N-phenylpropyl carboxamide 9 k (IC(50) =8.8 μM). Compound 9 k possesses selectivity toward HCV1b replicon Ava.5 cells (EC(50) =17.5 μM) over parent Huh-7 cells (CC(50) =187.5 μM). Compound 9 k effects a mixed mode of NS5B inhibition, with NTP-competitive displacement properties. The interaction between 9 k and NS5B is stabilized by the presence of magnesium ions. Docking studies showed that the binding orientation of 9 k occupies the central portions of both magnesium-mediated and NTP-ribose-response binding sites within the active site region of NS5B. As a result, 3-hydroxy-4-oxo-3,4-dihydroquinazolin-2-carboxamide derivatives are disclosed herein as novel, mainly active site inhibitors of HCV NS5B polymerase. 相似文献