Synthesis of the New Ring System Bispyrido[4',3':4,5]pyrrolo[1,2-a:1',2'-d]pyrazine and Its Deaza Analogue

Molecules

Barbara Parrino¹  Virginia Spanò¹  Anna Carbone¹  Paola Barraja¹  Patrizia Diana¹  Girolamo Cirrincione¹ 

[1] id="af1-molecules-19-13342">Dipartimento di Scienze e Tecnologie Biologiche Chimiche e Farmaceutiche (STEBICEF), Università degli Studi di Palermo, Via Archirafi 32, 90123 Palermo, Ita

关键词: diketopiperazines;    plinabulin A;    bispyrido-pyrrolo-pyrazine;    pyrido-pyrrolo-pyrazino-indole;    antiproliferative activity;   

DOI  :  10.3390/molecules190913342

来源: mdpi

【 摘 要 】

Derivatives of the new ring systems bispyrido[4',3':4,5]pyrrolo[1,2-a:1',2'-d]pyrazine-6,13-dione and its deaza analogue pyrido[4'',3'':4',5']pyrrolo-[1',2':4,5]pyrazino[1,2-a]indole-6,13-dione were conveniently synthesized through a four-step sequence. Symmetrical derivatives of the former ring system were obtained through self condensation. On the other hand, condensation of 6-azaindole carboxylic acid with indole 2-carboxylic acid afforded the deaza analogue ring system. Derivatives of the title ring system were tested by the National Cancer Institute (Bethesda, MD, USA) and four of them exhibited modest activity against MCF7 (a breast cancer cell line) and/or UO-31 (a renal cancer cell line).

【 授权许可】

CC BY   
© 2014 by the authors; licensee MDPI, Basel, Switzerland.