Ligand/PTC-free intramolecular Heck reaction: synthesis of pyrroloquinoxalines and their evaluation against PDE4/luciferase/oral cancer cell growth in vitro and zebrafish in vivo

被引：27

作者：

Babu, R. Vijaya ^{[1
,2
]}

Mukherjee, Soumita ^{[1
]}

Deora, Girdhar Singh ^{[1
]}

Chennubhotla, Keerthana Sarma ^{[1
,3
]}

Medisetti, Raghavender ^{[1
,3
]}

Yellanki, Swapna ^{[1
,3
]}

Kulkarni, Pushkar ^{[1
,3
]}

Sripelly, Shivashankar ^{[1
]}

Parsa, Kishore V. L. ^{[1
]}

Chatti, Kiranam ^{[1
]}

Mukkanti, K. ^{[2
]}

Pal, Manojit ^{[1
]}

机构：

[1] Univ Hyderabad Campus, Dr Reddys Inst Life Sci, Hyderabad 500046, Andhra Pradesh, India

[2] JNT Univ, Inst Sci & Technol, Dept Chem, Hyderabad 500072, Andhra Pradesh, India

[3] Univ Hyderabad Campus, Zephase Therapeut, Hyderabad 500046, Andhra Pradesh, India

来源：

ORGANIC & BIOMOLECULAR CHEMISTRY | 2013年 / 11卷 / 39期

关键词：

INHIBITORS; APOPTOSIS; STRATEGY; DESIGN; ASSAY;

D O I：

10.1039/c3ob41504j

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A series of 1,3-disubstituted pyrrolo[2,3-d]quinoxalines has been designed for the potential inhibition of PDE4 without inhibiting luciferase. A ligand/PTC (phase transfer catalyst) free intramolecular Heck cyclization strategy was used to prepare these compounds, some of which showed significant inhibition of PDE4B (IC50 approximate to 5-14 mu M) and growth inhibition of oral cancer cells (CAL 27) but not inhibition of luciferase in vitro. They also showed acceptable safety profiles but no apoptosis in zebrafish embryos.

引用

页码：6680 / 6685

页数：6

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