4705-39-9Relevant articles and documents
Synthesis of novel strobilurin-pyrimidine derivatives and their antiproliferative activity against human cancer cell lines
Chai, Baoshan,Wang, Shuyang,Yu, Wenquan,Li, Huichao,Song, Chuanjun,Xu, Ying,Liu, Changling,Chang, Junbiao
, p. 3505 - 3510 (2013/07/28)
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.
Synthesis and antitumor activities of a new series of 4,5-dihydro-1H- thiochromeno[4,3-d]pyrimidine derivatives
Guo, Dexiang,Liu, Yajing,Li, Ting,Wang, Nan,Zhai, Xin,Hu, Chun,Gong, Ping
experimental part, p. 347 - 351 (2012/08/08)
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.
Amidination of amines under microwave conditions using recyclable polymer-bound 1H-pyrazole-1-carboxamidine
Solodenko, Wladimir,Broeker, Patrick,Messinger, Josef,Schoen, Uwe,Kirschning, Andreas
, p. 461 - 466 (2007/10/03)
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.
