- Synthesis of novel strobilurin-pyrimidine derivatives and their antiproliferative activity against human cancer cell lines
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A series of new strobilurin-pyrimidine analogs were designed and synthesized based on the structures of our previously discovered antiproliferative compounds I and II. Biological evaluation with two human cancer cell lines (A549 and HL60) showed that most of these compounds possessed moderate to potent antiproliferative activity. Two potent candidates (8f, IC50 = 2.2 nM and 11d, IC50 = 3.4 nM) were identified with nanomolar activity against leukemia cancer cell line HL60 for further development. This activity represents a 1000- to 2500-fold improvement compared to the parent compounds I and II and is 20- to 30-fold better than the chemotherapy drug, doxorubicin. The present work provides strong incentive for further development of these strobilurin-pyrimidine analogs as potential antitumor agents for the treatment of leukemia.
- Chai, Baoshan,Wang, Shuyang,Yu, Wenquan,Li, Huichao,Song, Chuanjun,Xu, Ying,Liu, Changling,Chang, Junbiao
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p. 3505 - 3510
(2013/07/28)
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- Synthesis and antitumor activities of a new series of 4,5-dihydro-1H- thiochromeno[4,3-d]pyrimidine derivatives
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A new series of 4,5-dihydro-1H-thiochromeno[4,3-d ]pyrimidine derivatives have been designed and synthesized. The antitumor activities of the target compounds have been evaluated in vitro against two human cancer cell lines including A549 (human alveolar adenocarcinoma cell) and H460 (human lung cancer) by MTT assay. Most of the target compounds exhibited significant antitumor activities against A549 and H460 cancer cell lines. The most potent compound 4-(benzo[d][1,3]dioxol-5-yl)-8,9-difluoro-2-(4-methylpiperazin-1-yl)-4, 5-dihydro-1H-thiochromeno[4,3-d]pyrimidine (CH05) (IC50 = 0.44 μM, 3.07 μM) was 2.0 and 8.4 times more active than gefitinib (IC50 = 0.89 μM, 16.81 μM) against A549 and H460 cell lines, respectively.
- Guo, Dexiang,Liu, Yajing,Li, Ting,Wang, Nan,Zhai, Xin,Hu, Chun,Gong, Ping
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experimental part
p. 347 - 351
(2012/08/08)
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- Orthoamides and iminium salts, LXXX [1]. C-Glycosyl alkynecarboxylic acid orthoamides. Versatile intermediates in the synthesis of new types of highly substituted C-Nucleoside analogs
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The C-glycosyl alkynecarboxylic acid orthoamides 22 and 23 are proposed as versatile precursors for the synthesis of new types of C-nucleoside analogs. The new synthetic strategy includes alkynylation of protected aldoses 13 or ketoses by Grignard ethynyl
- Drandarov, Konstantin,Kantlehner, Willi
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p. 699 - 716
(2012/11/07)
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- Synthesis and cytotoxic activity of 2,5-disubstituted pyrimido[5,4-c] quinoline derivatives
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A series of 2,5-disubstituted pyrimido[5,4-c]quinoline derivatives were synthesized and their cytotoxic activity against H460, HT-29 and MDA-MB-231 cell lines was evaluated in vitro. It was found that most of the tested compounds especially compound 17, s
- Zhang, Fan,Zhai, Xin,Chen, Li Juan,Qi, Jian Guo,Cui, Bo,Gu, Yu Cheng,Gong, Ping
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scheme or table
p. 1277 - 1280
(2012/01/06)
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- Amidination of amines under microwave conditions using recyclable polymer-bound 1H-pyrazole-1-carboxamidine
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A convenient one-step transformation of primary and secondary amines into the corresponding unprotected guanidines using 4-benzyl-3,5-dimethyl-1H- pyrazole-1-carboxamidine and its polymer-bound variant is described. The scopes and limitations of the method, the microwave-assistance of amidination as well as a recycling protocol are examined. Georg Thieme Verlag Stuttgart.
- Solodenko, Wladimir,Broeker, Patrick,Messinger, Josef,Schoen, Uwe,Kirschning, Andreas
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p. 461 - 466
(2007/10/03)
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- A new reagent and its polymer-supported variant for the amidination of amines
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New reagents for the high yielding amidination of primary and secondary amines are described. By attaching a benzyl substituent to the 3,5-dimethyl-1H-pyrazole-1-carboxamidine ring, a reagent 1 is obtained which allows easy work-up after amidination because of solubility of byproducts in organic solvents. In addition, the polystyrene-bound analogue 2 was prepared which allows amidination of various amines with high purity.
- Dr?ger, Gerald,Solodenko, Wladimir,Messinger, Josef,Sch?n, Uwe,Kirschning, Andreas
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p. 1401 - 1403
(2007/10/03)
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- Method of modifying wrinkles using guanidine derivatives
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The invention relates to wrinkling modifiers and anti-aging cosmetic compositions which each comprise a guanidine derivative represented by the following general formula (1): wherein is a heterocyclic group selected from azetidine, pyrrolidine, piperidine, piperazine or morpholine, and R1and R2are the same or different from each other and independently a hydrogen atom, or an alkyl, hydroxyl, hydroxyalkyl, carboxyl, carboxyalkyl or amidino group, or a salt thereof. The cosmetic compositions are excellent in the effects of suppressing wrinkling and of removing wrinkles and give users a pleasant feeling upon use.
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- Process for the manufacture of guanidines
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A process for the manufacture of a guanidine by amidination of a primary or secundary amine, which process comprises reacting the amine with a salt of 1-amidino-1,2,4-triazol with a strong acid.
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