Design and Synthesis of l-AryIpyrrolo[3,2-c]quinoline Derivatives as Potential Anticancer Agents

CNU IR > Pharmacy and Science > 2011 Taiwanese-Russian Organic, Medicinal and Bio Chemistry Interactions & PST Medicinal Chemistry Symposium > Item 310902800/24253

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Title:	Design and Synthesis of l-AryIpyrrolo[3,2-c]quinoline Derivatives as Potential Anticancer Agents
Authors:	Hsing-Wen Lu (呂幸紋) Chien-Chin Huang (黃建智) Yi-Ling Hsu (徐宜伶) Hao-Lun Huang (黃皓倫) Hua-An Lin (林花安) Chun-Tang Chiou (邱俊棠) Grace Shiahuy Chen (陳香惠)
Date:	2011
Issue Date:	2011-06-23 14:57:38 (UTC+8)
Abstract:	Combrestastatin A4 (CA-4) is a well known potent tubulin polymerization inhibitor. It is structurally similar to colchicines and competes on the position of microtubule with colchicines. The structural features of CA-4 possess two aryl rings in the cis conformation with methoxy groups on the aryl rings. The derivatives of CA-4 have been proved to have great inhibitor activity against tublin polymerization. Quinoline derivatives have great biological activities in many aspects, and our results have shown that quinazoline derivatives with anilino substituents on the 2-position exhibited good anticancer activity. A benzoyl group was introduced onto the 4-position of quinazoline to mimic CA-4. However, our results showed that even methoxy groups introduced onto the benzoyl moiety and 6,7-position of quinazoline could not achieve a good anticancer activity, it was reasoned that the two aromatic conformation. Therefore, derivatives of l-arylpyrrolo[3,2-c]quinoline were designed to force the two aromatic rings in cis conformations. The biological results showed that 3-OMe, 4-OMe, 3,4-OMe and 3-OH-4-OMe on the 1-phenyl group played an important role in l_aryl_4-methyl-2,3-dihydropyrrolo[3,2-c]quinoline derivatives. The aromatic planar structure is assumed essential to the inhibitory activity. We hope that the results presented here will promote further research on this series of compounds as potential anticancer therapeutic agents.
Relation:	2011年台俄有機、藥物與生物化學交流暨藥物化學研討會，起迄日：2011/04/06~2011/04/05，地點：溪頭台大實驗林
Appears in Collections:	[Pharmacy and Science] 2011 Taiwanese-Russian Organic, Medicinal and Bio Chemistry Interactions & PST Medicinal Chemistry Symposium

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