含有生物活性吡唑部分的新型抗肿瘤乙酰胺、吡咯、吡咯并嘧啶、硫氰酸盐、腙、吡唑、异硫氰酸盐和噻吩衍生物。

Novel antitumor acetamide, pyrrole, pyrrolopyrimidine, thiocyanate, hydrazone, pyrazole, isothiocyanate and thiophene derivatives containing a biologically active pyrazole moiety.

作者信息

Alqasoumi Saleh I, Ghorab Moustafa M, Ismail Zeinab H, Abdel-Gawad Soad M, El-Gaby Mohamed S A, Aly Hala M

机构信息

Medicinal, Aromatic and Poisonous Plants Research Center (MAPPRC), College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.

出版信息

Arzneimittelforschung. 2009;59(12):666-71. doi: 10.1055/s-0031-1296457.

DOI:10.1055/s-0031-1296457

PMID:20108654

Abstract

4-Amino-N-(1-phenyl-1H-pyrazol-5-yl)-benzenesulfonamide (sulfaphenazole) 1 was selected as strategic starting material for the synthesis of some novel acetamide 2, pyrrole 4, pyrrolo[2,3-d]pyrimidine 5, thiocyanate 6, hydrazone 7a,b pyrazole 8, isothiocyanate 9 and thiophene 12 derivatives to evaluate theantitumor activity. Compound 4 was more effective than the reference drug, doxorubicin (CAS 23214-92-8) as positive control.

摘要

4-氨基-N-(1-苯基-1H-吡唑-5-基)苯磺酰胺（磺胺苯吡唑）1被选为合成一些新型乙酰胺2、吡咯4、吡咯并[2,3-d]嘧啶5、硫氰酸盐6、腙7a,b、吡唑8、异硫氰酸盐9和噻吩12衍生物的关键起始原料，以评估其抗肿瘤活性。化合物4比作为阳性对照的参比药物阿霉素（CAS 23214-92-8）更有效。