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Indole derivatives (2010–2020) as versatile tubulin inhibitors: synthesis and structure–activity relationships

Department of Chemistry, School of Chemical & Lifescience, Jamia Hamdard, New Delhi, 110062, India

Department of Pharmaceutical Chemistry, DPSRU, New Delhi, 110017, India

Department of Pharmaceutical Chemistry, School of Pharmaceutical Education & Research, Jamia Hamdard, New Delhi, 110062, India

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Syed Shafi

https://orcid.org/0000-0001-7657-0630

Department of Chemistry, School of Chemical & Lifescience, Jamia Hamdard, New Delhi, 110062, India

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Published Online:1 Sep 2021https://doi.org/10.4155/fmc-2020-0385

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Abstract

Tubulin inhibitors are conjugates that interfere with the dynamic equilibrium of the polymerization and depolymerization of microtubules. Among all the reported conjugates, indole moiety is one of the most significant classes for the development of new drug candidates for cancer therapy. Due to their presence in a wide range of natural as well as synthetic antitubulin agents, indole has become a versatile scaffold in research, and various synthetic and semisynthetic indole-based antitubulin agents have been identified and reported. The present article focuses on the reported indole-based tubulin inhibitors of synthetic origin from last the decade. Synthesis, structure–activity relationships and biological activities of synthetic indole derivatives along with brief updates on their antitubulin activity are presented.

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Vol. 13, No. 20

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Received 21 December 2020

Accepted 30 July 2021

Published online 1 September 2021

Published in print October 2021

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The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

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