Aim To design and synthesize a series of 2-（E）-（4-cyclopentyloxy-3-methoxylbenzylidene）cyclopentanone derivatives, and to determine their antitumor activities in vitro. Method The target compounds were synthesized...Aim To design and synthesize a series of 2-（E）-（4-cyclopentyloxy-3-methoxylbenzylidene）cyclopentanone derivatives, and to determine their antitumor activities in vitro. Method The target compounds were synthesized. Their antitumor activities were assayed using human hepatic carcinoma ceil line （Bel-7402） and human oral cavity epidermis squamoceilular carcinoma cell line （KB）. Results Five compounds were obtained. Three of them were not reported in the literature and their chemical structures were confirmed by IR, ^1H NMR, MS and elemental analysis. Preliminary screening results showed that compound 5 possessed better biological activity with IC50 1.62 μmol·L^-1 against Bel-7402 and 8.04 μmol·L^-1 against KB, but much weaker than 5- Fluorouracil. Conclusion Mannich base derivatives of 2-（E）-（4-cyclopentyloxy-3-methoxylbenzylidene）cyclopentanone exhibited some antitumor activities.展开更多
A series of alditol derivatives were designed and synthesized with relatively high yield. On the basis of reaction between sorbitol and a series of substituted benzaldehyde in the presence of an acid catalyst, a serie...A series of alditol derivatives were designed and synthesized with relatively high yield. On the basis of reaction between sorbitol and a series of substituted benzaldehyde in the presence of an acid catalyst, a series of acetal derivatives were synthesized through free hydroxyl esterification. D-sorbitol acetal amido derivatives were prepared by reduction of nitryl and acylation of amino. D-sorbitol acetal carboxyl esterification derivatives were prepared through esterification and hydrolysis. By high performance liquid chromatography-mass spectra (HPLC-MS) and 1H nuclear magnetic resonance spectra (1H-NMR), 36 compounds prepared were identified. Among these derivatives prepared, 26 compounds have not been reported in the previous literatures.展开更多
As benzoxazin-4-ones and quinazolines linked to indole nucleus acting as a good pharmacophore, the synthesis of these compounds has significant meaning. The key intermediates 2-（2＇, 5＇-disubstituted-indol-2＇-yl...As benzoxazin-4-ones and quinazolines linked to indole nucleus acting as a good pharmacophore, the synthesis of these compounds has significant meaning. The key intermediates 2-（2＇, 5＇-disubstituted-indol-2＇-yl）-4H-3, 1-benzoxazin-4-ones （3） were synthesized from cyclocondensation of indole-2-carbonyl chlorides （2） and anthranilic acid. Compound （3） on reaction with thiosemicarbazide and o-phenylene diamine afforded the compound （4） and （6） respectively. Compound （4） subjected to intramolecular cyclization under thermal conditions above its melting point afforded the compound （5）. Similarly compound （3） on fusion with o- phenylene diamine gave compound （7）. Structures of these compounds were confirmed by their spectral studies. The compounds were screened for their antimicrobial activity and the results were reported.展开更多
基金Natural Science Foundation of GuangdongProvince(Grant No.994615).
文摘Aim To design and synthesize a series of 2-（E）-（4-cyclopentyloxy-3-methoxylbenzylidene）cyclopentanone derivatives, and to determine their antitumor activities in vitro. Method The target compounds were synthesized. Their antitumor activities were assayed using human hepatic carcinoma ceil line （Bel-7402） and human oral cavity epidermis squamoceilular carcinoma cell line （KB）. Results Five compounds were obtained. Three of them were not reported in the literature and their chemical structures were confirmed by IR, ^1H NMR, MS and elemental analysis. Preliminary screening results showed that compound 5 possessed better biological activity with IC50 1.62 μmol·L^-1 against Bel-7402 and 8.04 μmol·L^-1 against KB, but much weaker than 5- Fluorouracil. Conclusion Mannich base derivatives of 2-（E）-（4-cyclopentyloxy-3-methoxylbenzylidene）cyclopentanone exhibited some antitumor activities.
基金National Natural Science Foundation of China (No 20306022)
文摘A series of alditol derivatives were designed and synthesized with relatively high yield. On the basis of reaction between sorbitol and a series of substituted benzaldehyde in the presence of an acid catalyst, a series of acetal derivatives were synthesized through free hydroxyl esterification. D-sorbitol acetal amido derivatives were prepared by reduction of nitryl and acylation of amino. D-sorbitol acetal carboxyl esterification derivatives were prepared through esterification and hydrolysis. By high performance liquid chromatography-mass spectra (HPLC-MS) and 1H nuclear magnetic resonance spectra (1H-NMR), 36 compounds prepared were identified. Among these derivatives prepared, 26 compounds have not been reported in the previous literatures.
文摘As benzoxazin-4-ones and quinazolines linked to indole nucleus acting as a good pharmacophore, the synthesis of these compounds has significant meaning. The key intermediates 2-（2＇, 5＇-disubstituted-indol-2＇-yl）-4H-3, 1-benzoxazin-4-ones （3） were synthesized from cyclocondensation of indole-2-carbonyl chlorides （2） and anthranilic acid. Compound （3） on reaction with thiosemicarbazide and o-phenylene diamine afforded the compound （4） and （6） respectively. Compound （4） subjected to intramolecular cyclization under thermal conditions above its melting point afforded the compound （5）. Similarly compound （3） on fusion with o- phenylene diamine gave compound （7）. Structures of these compounds were confirmed by their spectral studies. The compounds were screened for their antimicrobial activity and the results were reported.
