Synthesis and cytotoxic activity of novel quinazolino-β-carboline-5-one derivatives

• Published in: Bioorganic & medicinal chemistry Vol. 12; no. 9; pp. 1991 - 1994
• Main Authors: Baruah, Bipul, Dasu, Kavitha, Vaitilingam, Balasubramanian, Mamnoor, Premkumar, Venkata, Prasanthi Penubaka, Rajagopal, Sriram, Yeleswarapu, Koteswar Rao
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 01.05.2004; Elsevier Science
• Subjects: Animals; Antineoplastic agents; Antineoplastic Agents - chemical synthesis; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Biological and medical sciences; Carbolines - chemical synthesis; Carbolines - chemistry; Carbolines - pharmacology; Cell Line, Tumor; Cytotoxic; General aspects; Humans; Medical sciences; Mice; Mice, Nude; Neoplasm Transplantation; Pharmacology. Drug treatments; Quinazolines - chemistry; Quinazolino-β-carboline-5-one derivatives; Cytotoxic; Quinazolino-β-carboline-5-one derivatives; Antineoplastic agent; Pentacyclic compound; Angular nitrogen heterocycle; Rodentia; Lactam; Cytotoxicity; In vitro; In vivo; Vertebrata; Experimental disease; Mammalia; Cell line; Structure activity relation; Mouse; Animal; Colon; Chemical synthesis
• ISSN: 0968-0896; 1464-3391
• DOI: 10.1016/j.bmc.2004.03.005

Graphic A novel series of quinazolino-β-carbolinone derivatives was synthesized and evaluated for their in vitro and in vivo anticancer activity. Many compounds have shown good in vitro activity in the range 1–8 μM concentration. Three of the compounds were further tested in nude mice bearing HT-29 colon cancer xenografts.