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3-氰基-4,6-二取代-2(1H)-亚氨基或氧代吡啶：对白血病细胞系具有高选择性的新型抗肿瘤药物。

3-Cyano-4,6-disubstituted-2(1H)-imino or oxopyridines: new antineoplastic agents with high selectivity towards leukemia cell lines.

作者信息

Abadi A H, al-Khamees H A

机构信息

Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.

出版信息

Arch Pharm (Weinheim). 1998 Oct;331(10):319-24. doi: 10.1002/(sici)1521-4184(199810)331:10<319::aid-ardp319>3.3.co;2-m.

DOI:10.1002/(sici)1521-4184(199810)331:10<319::aid-ardp319>3.3.co;2-m
PMID:9844579
Abstract

Two series of 3-cyano-2(1H)-oxopyridine and 3-cyano-2(1H)-iminopyridine derivatives carrying various aryl substituents at position 4 and (4-((7-chloro or trifluoromethylquinol-4-yl)amino)phenyl) substituent at position 6 were synthesized and evaluated for their antitumor activity. Compounds 3f and 6d showed high selectivity towards leukemia cell lines with full panel median growth inhibition GI50 average sensitivity towards all cell lines (MG-MID) at 7.9 and 19.7 microM and leukemia subpanel GI50 average sensitivity towards leukemia cell lines (MG-MID) at 1.74 and 2.9 microM, respectively, also they exhibited full panel total growth inhibition TGI (MG-MID) at 34.8 and 59.0 microM and leukemia subpanel TGI (MG-MID) at 5.3 and 13.5 microM, respectively.

摘要

合成了两系列在4位带有各种芳基取代基且在6位带有(4-((7-氯或三氟甲基喹啉-4-基)氨基)phenyl)取代基的3-氰基-2(1H)-氧代吡啶和3-氰基-2(1H)-亚氨基吡啶衍生物，并对其抗肿瘤活性进行了评估。化合物3f和6d对白血病细胞系表现出高选择性，全细胞系中位生长抑制GI50（对所有细胞系的平均敏感性，MG-MID）分别为7.9和19.7微摩尔，白血病亚组GI50（对白血病细胞系的平均敏感性，MG-MID）分别为1.74和2.9微摩尔，它们还分别在34.8和59.0微摩尔表现出全细胞系总生长抑制TGI（MG-MID）以及在5.3和13.5微摩尔表现出白血病亚组TGI（MG-MID）。

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