PMID: 26899186Feb 24, 2016Paper

Recent Advances in Heterocyclic Tubulin Inhibitors Targeting the Colchicine Binding Site

Anti-cancer Agents in Medicinal Chemistry
Xiaoxin WuWei Li

Abstract

Microtubules are involved in many critical cellular processes including cell division, cell shape maintenance, vesicle transportation and motility regulation. Disruption of tubulin dynamics is a well-validated cancer drug target with several FDA approved, highly efficacious tubulin inhibitors targeting the taxane or the vinca binding sites. Despite the tremendous successes for these clinical tubulin inhibitors, their limitations are also apparent, particularly in the development of transporter mediated drug resistance. While currently there are no FDA approved inhibitors targeting the colchicine binding site in tubulin, extensive preclinical studies have suggested that colchicine binding site inhibitors (CBSIs) have significantly less susceptibility to transporter medicated drug resistance. The presence of one or more heterocyclic moieties is often critical for the antiproliferative activities for most of these CBSIs. This article aims to review the structures and antiproliferative activities of most recently developed heterocyclic CBSIs from 2013 to present. We focus this review on compounds that are designed based on the CA-4, chalcone and PTOX scaffolds which are well established to interact with the colchicine binding site ...Continue Reading

Citations

May 22, 2018·Future Medicinal Chemistry·Nehal M El-BakhshawangyAzza T Taher
Feb 13, 2019·Medicinal Research Reviews·Kinsie E ArnstDuane D Miller
Jan 25, 2019·Journal of Experimental & Clinical Cancer Research : CR·Vivek K KashyapSubhash C Chauhan
Jun 19, 2019·Current Topics in Medicinal Chemistry·Yongtao DuanChuanjun Song
Jul 30, 2019·Expert Opinion on Therapeutic Patents·Kashif HaiderAhmed Kamal
Dec 6, 2016·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Cristina C RohenaSusan L Mooberry
Apr 25, 2017·Critical Reviews in Biotechnology·Kashyap Kumar DubeyPratyoosh Shukla
Jul 28, 2020·Current Pharmaceutical Design·Georgios PremetisNikolaos E Labrou

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