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Discovery and development of synthetic tricyclic pyrroloquinone (TPQ) alkaloid analogs for human cancer

Wei Wang,Bhavitavya Nijampatnam,Sadanandan E. Velu,Ruiwen Zhang

《化学科学与工程前沿（英文）》 2016年第10卷第1期页码 1-15 doi: 10.1007/s11705-016-1562-6

摘要： Natural products and their derivatives represent a rich source for the discovery and development of new cancer therapeutic drugs. Bioactive components derived from natural sources including marine compounds have been shown to be effective agents in the clinic or in preclinical settings. In the present review, we present a story of discovery, synthesis and evaluation of three synthetic tricyclic pyrroloquinone (TPQ) alkaloid analogs as cancer therapeutic agents. Chemical synthesis of these compounds (BA-TPQ, TBA-TPQ, and TCBA-TPQ) has been accomplished and the mechanisms of action (MOA) and structure-activity relationships (SAR) have been investigated. In the past, the complexity of chemical synthesis and the lack of well-defined MOA have dampened the enthusiasm for the development of some makaluvamines. Recent discovery of novel molecular targets for these alkaloids (unrelated to inhibition of Topoisomerase II) warrant further consideration as clinical candidates in the future. In addition to the establishment of novel synthetic approaches and demonstration of and anticancer activities, we have successfully demonstrated that these makaluvamines attack several key molecular targets, including the MDM2-p53 pathway, providing ample opportunities of modulating the compound structure based on SAR and the use of such compounds in combination therapy in the future.

关键词： synthesis marine drugs tricyclic pyrroloquinone alkaloid cancer therapy MDM2 p53

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A highly efficient methodology for the preparation of

Yongxin Zhang, Shucheng Wang, Yaodong Huang

《化学科学与工程前沿（英文）》 2021年第15卷第3期页码 679-686 doi: 10.1007/s11705-020-1979-9

摘要： A convenient and highly efficient method is described for the synthesis of -methoxycarbazole derivatives, including those with sterically demanding, benzannulated, or strongly electron-donating or -withdrawing substituents. Various -methoxycarbazole derivatives were directly prepared in good-to-moderate yields by the Pd (dba) CHCl /9,9-dimethyl-4,5-bis(diphenylphosphino)xanthene-catalyzed reactions of the corresponding dibromobiphenyl compounds and methoxya-mine. Based on this methodology, the first total synthesis of 3,3′-[oxybis(methylene)]bis(9-methoxy-9 -carbazole), an antimicrobial dimeric carbazole alkaloid previously isolated from the stem bark of , was achieved in 18% yield over seven steps from 1,2-dibromobenzene.

关键词： N-methoxyl carbazole dimeric N-methoxyl carbazole alkaloid total synthesis double N-arylation of methoxyamine