A good strategy was brought forward for designing efficient haptens and complete antigens for 3-amino-2-oxazolidinone (AOZ). Haptens designed newly were achieved facilely in good yield by using LiCI-N(Et)3 as new ...A good strategy was brought forward for designing efficient haptens and complete antigens for 3-amino-2-oxazolidinone (AOZ). Haptens designed newly were achieved facilely in good yield by using LiCI-N(Et)3 as new catalysis system, the structure of which was elucidated by spectroscopy analysis, such as NMR and MS. Novel antigens for AOZ were prepared successfully by convenient active ester method. The ratios of haptens 3 and 4 to carrier proteins were proven respectively as 41 : 1 (5a), 39:1 (6a), 11:1 (5b) and 9:1 (6b) by trinitrobenzene sulfonic acid (TNBS) method. The results of indirect competitive ELISA (ic-ELISA) of antiserums indicated that the haptens with a short unsaturated side chain can evoke specific immune response effectively.展开更多
The reactions of tanshinone IIA with aromatic aldehydes have been investigated and several 2, T-(substituted arylmethylene) bis (1,6,6-trimethyl-6,7,8,9-tetrahydrophenanthro[1,2-b]- furan- 10, 11-dione) derivative...The reactions of tanshinone IIA with aromatic aldehydes have been investigated and several 2, T-(substituted arylmethylene) bis (1,6,6-trimethyl-6,7,8,9-tetrahydrophenanthro[1,2-b]- furan- 10, 11-dione) derivatives were obtained,展开更多
1-[1-(Benzyloxy)-3-methylnaphthalen-4-yloxy]propan-2-one (la) took place a cyclization, debenzylation and oxidation to form 9-substitued benzo[de]chromene-7,8-dione (2a) and 5-benzyl-9-substitued benzo[de]chrome...1-[1-(Benzyloxy)-3-methylnaphthalen-4-yloxy]propan-2-one (la) took place a cyclization, debenzylation and oxidation to form 9-substitued benzo[de]chromene-7,8-dione (2a) and 5-benzyl-9-substitued benzo[de]chromene-7,8-dione (3a). The mechanisms for these reactions were discussed.展开更多
A new bisbenzofuran analogue Ⅶ was achieved unexpectedly in one step procedure from 1-(4-methoxyphenoxy)acetone Ⅰ by using Amberlyst 15 resin as catalyst in excellent yield. The structure was elucidated by spectro...A new bisbenzofuran analogue Ⅶ was achieved unexpectedly in one step procedure from 1-(4-methoxyphenoxy)acetone Ⅰ by using Amberlyst 15 resin as catalyst in excellent yield. The structure was elucidated by spectroscopy analysis including ^1H-NMR, ^13C-NMR, DEPT, ESI-MS, element analysis.展开更多
A series of novel phenoxazinone derivatives (1-6) were designed and synthesized for evaluating their antitumor activities. The antiproliferative activities of the prepared compounds against representative human neop...A series of novel phenoxazinone derivatives (1-6) were designed and synthesized for evaluating their antitumor activities. The antiproliferative activities of the prepared compounds against representative human neoplastic cell lines were evaluated by MTF assay. The results showed that most of them inhibited cell proliferation in a submicromolar to rnicromolar range. These compounds were also evaluated against KBv200 and MCF-7/Adr cell lines, which overexpress the MDR/P-glycoprotein drug efflux pump responsible for drug resistance, and had a more potential for resisting MDR than their lead compound APO.展开更多
The reaction of cryptotanshinone and tanshinone IIA with several biogenic amine metabolites involved in the pathogenic pathways of HE were investigated and eight 1,2,3,4- tetrahydrophenanthrene derivatives, 2-6 and 8-...The reaction of cryptotanshinone and tanshinone IIA with several biogenic amine metabolites involved in the pathogenic pathways of HE were investigated and eight 1,2,3,4- tetrahydrophenanthrene derivatives, 2-6 and 8-10, were obtained. The probable mechanism on reaction was discussed.展开更多
A new approach to the facile synthesis of 2-substituted-quinazolin-4(3H)-ones and its derivatives using the condensation reaction of substituted 2-aminobenzamide and orthoesters is reported.
文摘A good strategy was brought forward for designing efficient haptens and complete antigens for 3-amino-2-oxazolidinone (AOZ). Haptens designed newly were achieved facilely in good yield by using LiCI-N(Et)3 as new catalysis system, the structure of which was elucidated by spectroscopy analysis, such as NMR and MS. Novel antigens for AOZ were prepared successfully by convenient active ester method. The ratios of haptens 3 and 4 to carrier proteins were proven respectively as 41 : 1 (5a), 39:1 (6a), 11:1 (5b) and 9:1 (6b) by trinitrobenzene sulfonic acid (TNBS) method. The results of indirect competitive ELISA (ic-ELISA) of antiserums indicated that the haptens with a short unsaturated side chain can evoke specific immune response effectively.
基金supported by Guangdong Natural Science Foundation and Guangzhou City Science Foundation(No.200221-E5011)
文摘The reactions of tanshinone IIA with aromatic aldehydes have been investigated and several 2, T-(substituted arylmethylene) bis (1,6,6-trimethyl-6,7,8,9-tetrahydrophenanthro[1,2-b]- furan- 10, 11-dione) derivatives were obtained,
基金We are indebted to the National Natural Science Foundation of China (No.20272085,20472117)the Guangzhou City Science Foundation,the Guangdong Provincial Science Foundation(031594)the Scientific Research Foundation for the Returned 0verseas Chinese Scholars,and the HongKong Polytechnic University Area of Strategic Development Fund for financial support of this study.
文摘1-[1-(Benzyloxy)-3-methylnaphthalen-4-yloxy]propan-2-one (la) took place a cyclization, debenzylation and oxidation to form 9-substitued benzo[de]chromene-7,8-dione (2a) and 5-benzyl-9-substitued benzo[de]chromene-7,8-dione (3a). The mechanisms for these reactions were discussed.
基金supported by the National Natural Science Foundation of China(20472117,20272085)the Natural Science Foundation of Guangdong Province(031594).
文摘A new bisbenzofuran analogue Ⅶ was achieved unexpectedly in one step procedure from 1-(4-methoxyphenoxy)acetone Ⅰ by using Amberlyst 15 resin as catalyst in excellent yield. The structure was elucidated by spectroscopy analysis including ^1H-NMR, ^13C-NMR, DEPT, ESI-MS, element analysis.
基金support by the National Natural Science Foundation of China(No.20472117)the Science Foundation of Zhuhai(PC20041131)the Scientific Research Foundation for the Returned 0verseas Chinese Scholars.
文摘A series of novel phenoxazinone derivatives (1-6) were designed and synthesized for evaluating their antitumor activities. The antiproliferative activities of the prepared compounds against representative human neoplastic cell lines were evaluated by MTF assay. The results showed that most of them inhibited cell proliferation in a submicromolar to rnicromolar range. These compounds were also evaluated against KBv200 and MCF-7/Adr cell lines, which overexpress the MDR/P-glycoprotein drug efflux pump responsible for drug resistance, and had a more potential for resisting MDR than their lead compound APO.
基金The program is sponsored by the Guangzhou City Science Foundation(2000-Z-021-01)Guangdong Provincial Science Foundation(2KM04103S).
文摘The reaction of cryptotanshinone and tanshinone IIA with several biogenic amine metabolites involved in the pathogenic pathways of HE were investigated and eight 1,2,3,4- tetrahydrophenanthrene derivatives, 2-6 and 8-10, were obtained. The probable mechanism on reaction was discussed.
基金the Natural Science Foundation of China(Nos.U0832005,90813011,20772159,30801436)the Ministry of Education of the People's Republic of China(No.200805581163)+1 种基金the Guangdong Natural Science Foundation(No.8451008901000214)the Science Foundation of Guangzhou(No.2009A1-E011-6)for financial support of this study.
文摘A new approach to the facile synthesis of 2-substituted-quinazolin-4(3H)-ones and its derivatives using the condensation reaction of substituted 2-aminobenzamide and orthoesters is reported.